Organic synthesis of bioactive molecules

This paper presents findings on polyethyleneimine (PEI) impregnation on palm shell activated carbon (AC) with regards to effects of impregnation amount and types of PEI used on surface characteristics as well as metal ions adsorption capacities of the AC. Fundamental interactions between PEI molecules and metal ions on textural surface (micro-and mesopores) of the AC are elucidated. Three types of low molecular weight PEI distinguished by their molecular numbers, Mn (423, 600 and 1200) are used for the impregnation process. Impregnation at 8.41 wt% 423-PEI/AC provides optimum increases for nickel and copper adsorption capacities by factors of 2.6 and 1.5 respectively at 49% reduction of Brunauer-Emmett-Teller (BET) surface area as compared to virgin AC. Only 423-PEI molecules are shown to have considerably filled the micropores of AC whereas the 600-and 1200-PEI molecules are too large (in terms of molecular sizes) to infiltrate the micropores.

The present investigation was carried out to determine the possible bioactive components of tuber of Ruellia tuberosa L. (Acanthaceae) using GC-MS analysis. Twenty five compounds were identified. The prevailing compounds in the ethanol extract of tuber of R. tuberosa were Lupeol (68.14%), Stigmasterol (8.89%), á-Sitosterol (3.99%), Sucrose (2.24%), Cholest-5-ene, 3-bromo-, (3á- (2.24%), Octadecane, 2-methyl- (2.10%), Nonadecane, 2-methyl- (1.93%), Eicosane, 2-methyl- (1.79%) Heptacosane (1.43%) and Heptacosane (1.29%).

The effect of three tetrahydroxylated Schiff bases as N,N-bis(2,3-dihydroxybenzyl-idene)-4,4'-diphenylmethane, N,N-bis(2,4-dihydroxybenzyl-idene)-4,4'-diphenylmethane and N,N-bis(2,4-dihydroxybenzylidene)-4,4'-diphenylmethane were studied as inhibitors for mild steel in 1M HCl medium. The experiments were performed using potentiodynamic polarization. This inhibition proved an efficient increase according the position of second hydroxyl of salicylaldehyde suggesting that this inhibition is dependent on concentration and the compound nature. Among these position-isomers, the best inhibition efficiency was obtained with p-hydroxylated (94%) at 1mM. Tafel plots of these inhibitors are the mixed-type, their adsorption is spontaneous obeying to Langmuir's isotherm. AFM/SEM-EDS characterized metal surface. DFT-calculations and molecular dynamics simulations are correlated to inhibition efficiency obtained.

A copper-mediated Duff reaction for ortho-selective formylation of
phenols has been developed. In the presence of copper species, significant
improvements of yield and ortho-selectivity of the Duff formylation were achieved,
which provides an easy access to salicylaldehydes from phenols.

Starting from 2-imino-N-phenyl-2H-chromene-3-carbox-amide, (1) a series of functionalized chromenes were achieved; such as, 2-ethoxy-2,3-dihydro-3-phenylchromeno[2,3-d]pyrimidin-4-one (2), and 2-hydrazinyl-2,3-dihydro-3-phenylchromeno-[2,3-d]pyrimidin-4-one (3). Furthermore, reactions of (3) with some of laboratory available compounds gave pyrazoles (4 -9, 12, 13a, 13b), tetrazoles (11), 2-(2-benzylidenehydrazinyl)-3-phenyl-3H-chromeno[2,3-d]pyrimidin-4(10H)-oneisoxazoles , 5-chloro-1-(4-oxo-3-phenyl-4,10-dihydro-3H-chromeno[2,3-d]pyrimidin-2-yl)-3-phenyl-2, 3-dihydro-1H-pyrazole-4-carbonitrile (17), pyrimidines (28a, b), pyridines , benzo[b][1, 4]oxazepin-2-amines (32a, b), 3-chloro-4-(2-imino-2H-chromen-3-yl)-1-phenyl-4-(phenylamino) azetidin-2-one (34a-34e) and 2-(2-imino-2H-chromen-3-yl)-3-phenyl-2-(phenyl amino)thiazolidin-4-onee (35a -35e). The structures of these compounds were established by elemental analysis, IR, MS and NMR spectral analysis.

The carbonylation of unsaturated hydrocarbons, alcohols,
organic halides and other substrates catalysed by transition
metals, salts of transition metals and organometallic
complexes is a widely used method for the synthesis of
new carbonyl-, carboxyl- and alkoxycarbonyl- containing
compounds including the creation or modification of
heterocycles.

A new series of pyrano-chromene and pyrimido pyrano-chromene derivatives were synthesized starting from 2-amino-4-(1-naphthyl)-5-oxo-4H,5H-pyrano[3,2-c]chromene-3-carbonitrile (6). The structures of the synthesized compounds were elucidated by spectral data. Compounds 6–11, 13–15 and 18 have been selected for their inhibitory activity screening against HIV-1 and HIV-2 in MT-4 cells.

The novel Schiff base ligand 2-(2-hydroxy-3-methoxybenzylidene)-N-(4-phenylthiazol-2-yl)hydrazinecarboxamide (L) obtained by the
condensation of N-(4-phenylthiazol-2-yl)hydrazinecarboxamide with o-vanillin and its Cu(II), Co(II), Ni(II) and Zn(II) complexes were
synthesized and characterized by elemental analysis and various physico-chemical techniques like, FT-IR, 1H NMR, ESI mass, UVVisible,
ESR, TGA/DTA, magnetic measurements and molar conductance. The spectral results confirmed tridentate ONO donor
binding of the ligand involving oxygen atom of amide carbonyl, azomethine nitrogen and oxygen of hydroxyl via deprotonation.
Spectral analysis indicates octahedral geometry for all the complexes. Co(II) complex has 1:1 stoichiometry ratio of the type
[M(L)(H2O)2Cl], whereas Cu(II), Ni(II) and Zn(II) complexes have 1:2 stoichiometric ratio of the type [M(L)2]. In order to evaluate the
effect of antimicrobial activity of metal ions upon chelation, all the newly synthesized compounds were screened for their
antibacterial and antifungal activities by minimum inhibitory concentration (MIC) method. The DNA cleavage activities were also
studied using plasmid DNA pBR322 as a target molecule.

Improvements over the Rothemund classical reaction methods have allowed the development of capacity to obtain a wide range of structures that were earlier unavailable. Performing the reaction in a mixed nitrobenzene/carboxylic acid medium allowed improvements of yield and purity of the porphyrin obtained, and in some cases the control of the oxidation level of the macrocycle. More recently, novel microwave synthetic methodologies were exploited to achieve important improvements in simple porphyrin chemistry. Tidy sulphonations of simple porphyrins opened the way to diverse desired, inexpensive structures in a very simple manner. The option to concentrate interests on improvements of synthetic methods to obtain simple and diversifi ed tetrapyrrolic structures proved to be advantageous. Interesting biomimetic oxidation and photooxidation systems and PDT sensitizers were developed and signifi cant knowledge was achieved in these specifi c and related areas. This review presents a view of our own results in the synthetic area, and outlines the contributions therefrom to the study of biomimetic and therapeutic processes.

This article presents a mini review of screened medicinal plants with promising wound healing potential from past and present documented literatures. Nature is a paradise of medicinal principles offer to the universe through plants that are highly rich in phytochemicals since the time immemorial. It is imperative to say that plants and humans have co-existed since the beginning of the world and in recent years, the screening of higher plants for unique biologically active compounds, particularly those that efficiently intervene in human illnesses has received the interest of the science community. Nevertheless, the use of traditional medicinal plant in most African countries is often associated with witchcraft and superstition, because people lack the scientific insight to explain the curative action of the plants. Wound is loss or break in anatomic stability of active tissue and it does not only pose physical and mental treat to zillions of people, but can also lead failure of multiple organs, amputation and even death. The wounded tissue is a perfect means for operation of contagion bacterial and the wounded area is consequently remain susceptible to aggressive microbes attack. The principal aim of screening medicinal plants for wound management is therefore to sort after natural healer that can accelerate the process of restoring the damaged tissue structure, strength and function and as well inhibit the probability of infections. The review, therefore, discuss about highly sorted medicinal plants that have demonstrated wound healing potential, the part used, wound healing efficacy, phytochemical role and references which will help future researchers to gain insight on next line of research in developing sound therapeutic new wound healing formulation for humanity purpose.

The qualities of polymer based biomaterials in facilitating bone regeneration process through tissue engi-neering have attracted the attention of researchers. Biomaterials with properties that can be manipulatedto mimic the three-dimensional architecture of extracellular matrix (ECM) of the native bone tissues, withmechanical properties required for scaffold, biodegradability, excellent biocompatibility and non-toxicityare required. The unique qualities of bacterial cellulose (BC) including biocompatibility, good mechanicalstrength, microporosity and biodegradability with its unique surface chemistry make it ideally suitablefor bone regeneration applications. The ease of being manipulated to mimic any form and structure makeit good scaffold biomaterial to incorporate other nanoparticles for cell proliferation and differentiationfor timely osseointegration and bone ingrowth. This review detailed requirements of scaffold materialsfor bone tissue engineering, provides comprehensive knowledge and highlights of current research onbacterial cellulose composites used for tissue engineering and the potentials of bacterial cellulose forbone regeneration including other nanoparticles incorporated.

An experiment was conducted at El-Bossily Protected Cultivation Experimental Farm, Central Laboratory for Agricultural Climate (CLAC), Agricultural Research Center (ARC), at Behaira Governorate, Egypt, during the autumn seasons of 2010/2011 and 2011/2012 to study the Economic considerations of using different types of organic manure on sweet pepper yield under protected cultivation (Vermicompost, compost and Cattle manure at the rates of 2, 4 and 6% (1.8, 3.6 and 5.4 m 3 /plastic house of 540m 2) were the organic fertilizer treatments. The study aimed to investigate increasing organic soil matter content in sandy soil by different rates and types of soil amendments as well as investigate their effects on vegetative growth and yield of sweet pepper using a split plot design with three replicates. Results obtained indicate that increasing rate of the different soil amendments from 1.8 to 5.4 m 3 /plastic house led to increase in vegetative growth and significantly enhanced early and t...

A new procedure to obtain anthracene-1,4-diones from p-benzoquinones and myrcene, in the presence of acids, is described. The cycloaddition reaction between α-myrcene and p-benzoquinones, followed by oxidation, led to 1,4-naphthoquinones or 1,4-anthraquinones depending upon whether the Lewis acid used in the Diels-Alder reaction, was present or absent during oxidation; furthermore, traces of acid in the solvents played an important role in determining the cycloadduct obtained. The quinones synthesized exhibited cytotoxicity towards several tumor cell lines.

Nature is the best source of medicines. Plants consisting of various types of organic substances,
and they impart different biological activities. The numerous medicines are administered to our
body though diets. These foods protect us from different types of diseases and disorders. Here
we planned to conduct phytochemical screening of the methanol extracts of Parmentiera
cereifera fruit. The outcomes of phytochemical screening of methanol extracts exhibited the
presence of flavonoids, saponins, tannins, triterpenoids as well as steroids. These
phytoconstituents are used in ailment of various diseases such as antipyretic, analgesic,
diabetes, cardioprotective, lipid lowering activity, hepatoprotective, antidiabetics, antidiarrhoeal,
anticancer, antiasthmatic activities, antimicrobial etc. These are only preliminary studies to isolate
potential compounds which may be use as a lead compound for several biological activities.

Computational modeling demonstrates that the van-der-Waals surfaces of homocubyl amines are similar to that of the neuroprotector Memantine Ò . Utilizing readily available precursors we report the preparation of a series of homological cubylamines, namely pentacyclo[6.3.0.0 2,6 .0 3,10 .0 5,9 ]undecyl-4-amine (trishomocubyl-4-amine, 2), pentacyclo[5.3.0.0 2,5 . 0 3,9 .0 4,8 ]decyl-10-amine (bishomocubyl-10-amine, 3), pentacyclo[4.3.0.0 2,5 .0 3,8 .0 4,7 ]nonyl-9-amine (homocubyl-9-amine, 4), and pentacyclo[4.2.0.0 2,5 .0 3,8 .0 4,7 ]octyl-1-amine (cubylamine, 5). The hydrochlorides of amines 2-5 show pronounced affinity for the (?)MK-801 channel binding site, and it seems likely that these compounds would act as very fast voltagedependent NMDA receptor antagonists.

A new series of N-acylhydrazone derivatives of 2-mercaptobenzimidazole (2-MBI) has been synthesized through S-alkylation with 1-bromotetradecane and N-alkylation with ethyl-2-chloroacetate. The resulting ester was synthetically modified through hydrazine hydrate to acyl hydrazide which was condensed with aromatic al-dehydes to afford the title N-acylhydrazones (4-17). Chemical structures of the newly synthesized compounds have been confirmed through mass, FT-IR and 1 HNMR techniques. In vitro free radical scavenging and α-glu-cosidase inhibition activities of the compounds were investigated with reference to the standard ascorbic acid and acarbose, respectively. Amongst the target compounds, 13 showed the highest inhibition in DPPH scavenging assay (IC 50 = 131.50 µM) and α-glucosidase inhibition potential (IC 50 = 352 µg/ml). We extended our investigations to explore the mechanism of enzyme inhibition and conducted docking analysis by using Molecular Operating Environment (MOE 2016.08). A homology model for α-glucosidase was constructed and validated using Ramachandran plot. Docking studies were also carried out on human intestinal α-glucosidases. In view of the importance of the nucleus involved, the synthesized compounds might find extensive medicinal applications as reported in the literature.

Objective: To determine chemical compositions, physicochemical properties and evaluating
antibacterial activities of essential oils extracted from leaves of Ocimum urticifolium (O.
urticifolium).
Methods: Essential oil of O. urticifolium was extracted by hydrodistillation technique. A
number of phytochemical screening tests were applied to identify the classes of compounds
in the leaves extract of O. urticifolium. Gas chromatography and gas chromatography/mass
spectrometry were used to characterize the chemical components in the essential oil. The agar
diffusion method was used to evaluate the antibacterial activity as per of standard procedure.
Results: Phytochemical screening of crude extract revealed that the presence of tannins,
glycosides, saponins, flavonoids, steroids, terpenoids and phenols. The obtained oil yield is
(0.33 ± 0.11) % (v/w). Analysis of oil using gas chromatography and gas chromatography/
mass spectrometry showed a total of 22 components, the abundance of monoterpene and
sesquiterpenes (98.99%). The percentage composition of monoterpene in the oil was α-pinene
(22.105%), eugenol (21.099%), while sesquiterpenes α-cubebene (11.341%), α-bisabolene
(9.945%), α-caryophyllene (7.709%), α-caryophyllene oxide (5.754%), and copaene (3.594%).
The oil inhibited the growth of Staphylococcus aureus and Escherichia coli, while no activity
was shown to Salmonella typhi.
Conclusions: The O. urticifolium is a rich source of various classes of chemical constituents
and the antibacterial activity of the oil could be attributed mainly to these compounds.

Guar gum is a galactomannan, obtained from plant Cyamopsis tetragonolobus (Leguminoceae). It has wide applications in Pharmaceutical formulations, Cosmetic, Food, Textile, Paper, Explosive, Toiletries industries etc. In pharmaceuticals, it is used as tablet binder and disintegrant, suspending, thickening and stabilising agent, as a controlled release carrier. Chemically guar gum is a hydrocolloidal polysaccharide composed of sugar galactose and mannose in molecular ratio of 1:1.4-1:2. Therapeutically it is used as hypoglycaemic, hypolipidemic, antimicrobial, antiproliferative, appetite suppressant, bulk forming laxative, in collitis and Crohn's disease etc. The present review renders elaborate potential data on the range of pharmaceutical, chemical, pharmacological and various industrial applications of guar gum.

Membrane Lipid Replacement (MLR) is the functional use of dietary supplements containing cell membrane glycerolphospholipids and antioxidants to safely replace and remove damaged membrane phospholipids that accumulate during various chronic and acute illnesses and during aging. Some products used in MLR are obtained from soy lecithin extracts that contain cell membrane glycerolphospholipids. Thus the soybean source has been questioned because of concerns related to genetic engineering (GMO) and the potential presence of hormone-like components and soy allergens. There is a complete absence of proteins, glycoproteins or carbohydrates in soy lecithins and MLR supplements that could be allergenic. One lecithin ingredient that contains purified membrane phospholipids (NTFactor Lipids®) has been shown to produce significant positive health benefits in clinical trials. NTFactor Lipids® are fractionated and purified from non-GMO soy lecithin, but this formulation does not contain detectable amounts of protein or glycoprotein allergens or other components that could elicit allergic or non-allergic adverse reactions. In addition, allergenic and non-allergenic reactions have not been found in multiple clinical trials and studies that have utilized this dietary supplement. NTFactor Lipids® are manufactured in certified Good Manufacturing Practices (cGMP) facilities using established allergen-control strategies to minimize any cross-contact with food allergens.

Keywords: Phospholipids, Clinical trials, Allergies, Cellular membranes

Methodology: Crude extract of Myristica fragrans seed was obtained using organic solvent (distilled water, ethyl acetate and ethanol) with solvent extraction technique and preliminary phytoconstituents was determined. The essential oil was extracted by hydrodistillation technique and isolated with petroleum ether. Metabolites present in the essential oil were quantified using Gas Chromatography Flame Ionization Detection (GCFID). Antifungal activity of Myristica fragrans oil and crude extract were investigated using agar well diffusion method. Folin-Ciocalteu and 2,2, diphenyl picryl hydrazyl (DPPH) radical scavenging assays were employed to determine total phenolic content and antioxidant activity respectively. Results: Preliminary phytochemical screening of Myristica fragrans seed revealed the existence of alkaloid, phenols, flavonoids, terpenes, saponins, glycosides, tannins, steroids and phenolic compounds. The percentage yield of Myristica fragrans oil extracted was 3.25%. Thirty-six metabolites were quantified in Myristica fragrans essential oil using GCFID among which are sabinene (26.58%), myristicin (13.55%), alpha-pinene (11.84%), terpinene-4-ol (9.35%), limonene (5.74%), safrole (5.40%), alpha-terpineol (4.51%), alpha-myrcena (3.82%), gama- terpinene (3.71%), alpha-terpinolene (3.19%), pinene-2-ol (1.84%), elimicin (1.27%) and isoeugenol (1.13%) respectively. Highest scavenging and antifungal activities were observed in ethyl acetate extract of Myristica fragrans compared to Beta-carotene and antifungal drug (Fluconazole) used as control at varying concentrations.  Conclusion: Presence of thirty-six different phytoconstituents (metabolites) in Myristica fragrans essential oil poses the potential of providing useful drugs for treating food-borne infection              and reduction of oxidative stress in the body other than its general uses as spices and flavoring agent.

Microbial hydroxylation of dydrogesterone (9,10-pregna-4,6diene-3,20-dione) (1) on fermentation with Rhizopus stolonifer afforded a new metabolite, 9,12-dihydroxy-9,10-pregna-4,6diene-3,20-dione (2). Its structure was deduced on the basis of modern spectroscopic techniques.

A magnetic multi-functional composite with a tri-layer core– shell– shell construction was successfully
prepared by a combination process involving click reactions and emulsion polymerization. Firstly,
magnetic polyxanthone triazole (PXT) was synthesized via the click reaction of bisethynyl and 2,7-(N -2-chloroacetamide) xanthone (NClX) in the presence of Fe3O 4 nanoparticles. Then, a
polypyrrole@polyxanthone triazole@Fe 3O4 (PPy@PXT@Fe3O4 ) tri-layered nanocomposite was prepared
via emulsion polymerization of pyrrole in the presence of magnetic PXT using sodium dodecyl sulfate
(SDS) as an emulsifier and ammonium persulfate (APS) as an oxidant. Characterization of the synthesized
polymer and nanocomposite was carried out by nuclear magnetic resonance (NMR), Fourier transform
infrared (FT-IR), X-ray diffraction (XRD), scanning electron microscopy (SEM), thermal gravimetric analysis
(TGA), Brunauer – Emmett– Teller (BET) survey, transmission electron microscopy (TEM) and vibrating
sample magnetometer (VSM) studies. Also, the antioxidant activity of the nanocomposites was examined
and compared with the bare polymer using a 2,2-diphenyl-1-picryl-hydrazyl free radical (DPPHc ) assay.
In addition, the in vitro antibacterial activities of the di-layered and tri-layered nanocomposites were
studied by inhibition zone methods. The results showed a greater synergic effect in the thermal stability,
antioxidant and antibacterial activities of the tri-layered nanocomposite than of the di-layered
nanocomposite. Thus, the developed PPy@PXT@Fe3O 4 tri-layered nanocomposite could be used
effectively for biomedical applications and would be a good sorbent candidate for the microbial
treatment of wastewater

Efficient synthetic methodology for preparation of 2-phosphiniminium-5-methylbenzenesulfonate zwitterions
is reported. Staudinger reaction between phosphines and n-propyl 2-azido-5-methylbenzenesulfonates
followed by sulfonate ester deprotection using pyridinium tetrafluoroborate/pyridine afforded the
zwitterions in excellent yields. This new route directly accesses ortho-substituted-arenesulfonate ligands
that incorporate a phosphinimine, a strong r-donor.

6-Hydroxy-2-oxo-2H-chromene-4-carbaldehyde (2), 6-chloro-2-oxo-2H-chromene-4-carbaldehyde (3) and 6-hydrazinyl-4-methyl-2H-chromen-2-one (5) were prepared as single-pharmacophore motif key intermediates. Compounds 2, 3 and 5 were incorporated in a series of multicomponent reactions (MCRs), under microwave assistance as well as conventional chemical synthesis processes, to afford a series of three and/or four-pharmacophoric-motif conjugates 8a,b, 11, 13, 16, 17, 19 and 20 in good yields. The newly synthesized compounds were characterized by IR, NMR, 13 C-NMR, MS and elemental analyses. Finally the synthesized compounds have been screened for their biological activity whereupon they exhibited remarkable antimicrobial activity on different classes of bacteria and the fungus.

Novel spiropyrrolizine / pyrrolidineoxindole moieties were synthesized chemo-, and
regio-selectively in high yields from knoevenagel reaction of bis[arylmethylidene]piperidin-4-ones,
isatin and L-proline or sarcosine under classical, ultrasonic, and microwave conditions. Seven
derivatives of the synthesized dispiro-pyrrolizidine-oxindole and spiropyrrolidine were screened
for their antitumor activity against two cell lines MCF-7 (breast cancer) and HEPG2 (liver cancer).
The results of biological activity indicated that the tested derivatives showed potent activity against
breast cancer cell MCF-7. Molecular docking simulation screening studies of the synthesized products with each of the receptors of (3hb5) for breast cancer and (4k9g) for liver cancer and their interaction with 1H5U of glycogen phosphorylase B, type 2 diabetes drug were examined. The docking
study of dispiro-pyrrolizidine-oxindole and spiropyrrolidine showed promising results with several
derivatives.

The current research examined the use of sodium tert butoxide as a catalyst for the synthesis of 2-(2-nitrovinyl) furan. The compound was synthesized via the condensation of furfural with nitromethane using sodium tert-butoxide as catalyst; unlike the ubiquitous use of sodium hydroxide, ethanol and isobutylamine as catalysts in which longer reaction time (five hours), reflux (heat) and strong agitation were required before getting to completion. In contrast with the use of the alkoxide as catalyst, the reaction went to completion with stirring for fifteen minutes. The product crystallized exclusively as the trans-isomer when the reaction was stopped by neutralizing the medium (base) with dilute hydrochloric acid. The compound was characterized using 1 H and 13 C Nuclear Magnetic Resonance (NMR) spectroscopy and melting point

The title compounds, C 12 H 10 N 3 O 7 SCl (I) and C 15 H 27 NO 3 S (II), crystallize in the monoclinic system, space group P2 1 /c with a = 7.3995(1), b = 27.8489(6), c = 9.8246(2) Å, β = 131.349(1)º, V = 1519.82(5) Å 3 , Z = 4, F(000) = 768, R int = 0.033 and S = 1.03 for I, and in the orthorhombic system, space group Pbca with a = 8.6227(1), b = 16.1480(4), c = 23.8774(6) Å, V = 3324.67(12) Å 3 , Z = 8, F(000) = 1312, R int = 0.024 and S = 1.04 for II. We have devised a convenient procedure for the synthesis of fused organic salts resulting from 1:1 proton-transfer, using an amine and a derivative of benzenesulfonic acid. The synthesized salts have a number of applications ranging from their consumption as eco-friendly solvents and catalysts in organic syntheses, to being used as efficient precursors for the production of sulfa drugs. Structures of compounds 3-chloroanilinium 2,4-dinitrobenzenesulfonate (CA-DNBS) and triethylaminium 2,4,6-trimethylbenzenesulfonate (TEA-TMBS) were determined by single-crystal X-ray diffraction studies and infrared spectroscopy.

The rearrangement of easily accessible Cookson's diketone with chlorosulfonic acid in chloroform followed by the acidic hydrolysis gave 6-chloro-7-hydroxy-dichloropentacyclo[6.3.0.0 2,6 .0 3,10 .0 5,9 ]undecane-4-one, whose syn-stereochemistry was assigned through the X-ray crystal structure analysis. This key structure was used for the stereoselective synthesis of the D 3 -trishomocubane derivatives as well as for the preparation of potential drugs bearing hydroxy-and amino-functional groups. A new multigram preparative synthesis of D 3 -trishomocubane was developed.

Metal-free 1,3-dipolar cycloaddition reactions have proven to be a powerful tool for the assembly of key heterocycles, in particular diversely functionalized 1,2,3-triazoles. A number of metal-free (3+2)-cycloaddition approaches have been developed up to date with the aim to circumvent the use of metal catalysts allowing these reactions to take place in biological systems without perturbation of the naturally occurring processes. This feature article specifically provides an overview of emerging metal-free synthetic routes, and their mechanistic features, in the formation of functionalized 1,2,3-triazoles.

5-Amino-3-(3-methyl-5-oxo-1-phenyl-2-pyrazolin-4-yl)-7-phenyl-7H-thiazolo[3,2-a]pyrimidine-6-carbonitrile was synthesized via the reaction of 4-(2-aminothiazol-4-yl)-3methyl-1-phenyl-2-pyrazolin-5-one with benzylidene malononitrile and was then transformed to related fused heterocyclic systems. The antifungal and antibacterial studies revealed in some cases excellent biocidal properties.

The Morita-Baylis-Hillman (MBH) reaction has attracted great
attention to generate densely functionalized adducts with
promising synthetic utility and biological activities. In this work
we demonstrate, for the first time, the synthesis of a series of
new lipophilic hydroxylated α-alkyl γ-nitroesters, advanced γ-
aminobutyric acid (GABA) intermediates, using the Morita-
Baylis-Hillman (MBH) reaction as key step. The results show that
the long-chain MBH adducts can be synthesized in good yields
in a metal-free organocatalytic system in the presence of
aliphatic aldehydes and activated alkenes, acrylonitrile or
methyl acrylate. Followed, the Michael addition of nitromethane
to MBH adducts resulted in hydroxylated α-alkyl γ-
nitroesters in good yields. Thus, the key MBH reaction led to
new lipophilic GABA advanced intermediates in good overall
yields from aliphatic aldehydes, demonstrating the potential of
this reaction pathway towards the synthesis of new drug
molecules for the treatment of psychiatric or neurodegenerative
disorders.

Traditional System-on-Chip (SoC) design employed shared buses for data transfer among various subsystems. As SoCs become more complex involving a larger number of subsystems, traditional bus-based architecture is giving way to a new paradigm for on-chip communication. This paradigm is called Network-on-Chip (NoC). A communication network of point-to-point links and routing switches is used to facilitate communication between subsystems. The routing switch proposed in this paper consists of four components, namely the input ports, output ports, switching fabric, and scheduler. The scheduler design is described in this paper. The function of the scheduler is to arbitrate between requests by data packets for use of the switching fabric. The scheduler uses an improved round robin based arbitration algorithm. Due to the symmetric structure of the scheduler, an area-efficient design is proposed by folding the scheduler onto itself, thereby reducing its area roughly by 50%.

A green and efficient procedure for the preparation of bis(indolyl)methanes via the condensation of indoles with various carbonyl compounds in the presence of catalytic amount of nanosilica gel under ultrasonic irradiation in good to excellent yields (83% to 94% ) in solvent-free condition is described. Short reaction time, easy and quick isolation of the products, environmentally friendly procedure, excellent chemoselectivity, and excellent yields are the main advantages of this procedure. Native nanosilica gel was used as an inexpensive and readily available catalyst without any support of reagent or modification on it. The reaction is carried out in solvent-free condition in the absence of ultrasonic irradiation at 80°C, too. This methodology offers significant improvements for the synthesis of bis(indolyl)methanes with regard to the yield of products, simplicity in operation, and green aspects by avoiding toxic catalysts and solvents. Recovery and recycling of the silica nanoparticle catalyst were also described.

An experiment was conducted at El-Bossily Protected Cultivation Experimental Farm, Central Laboratory for Agricultural Climate (CLAC), Agricultural Research Center (ARC), at Behaira Governorate, Egypt, during the autumn seasons of 2010/2011 and 2011/2012 to study the Economic considerations of using different types of organic manure on sweet pepper yield under protected cultivation (Vermicompost, compost and Cattle manure at the rates of 2, 4 and 6% (1.8, 3.6 and 5.4 m 3 /plastic house of 540m 2) were the organic fertilizer treatments. The study aimed to investigate increasing organic soil matter content in sandy soil by different rates and types of soil amendments as well as investigate their effects on vegetative growth and yield of sweet pepper using a split plot design with three replicates. Results obtained indicate that increasing rate of the different soil amendments from 1.8 to 5.4 m 3 /plastic house led to increase in vegetative growth and significantly enhanced early and t...

A new series of N-acylhydrazone derivatives of 2-mercaptobenzimidazole (2-MBI) has been synthesized through S-alkylation with 1-bromotetradecane and N-alkylation with ethyl-2-chloroacetate. The resulting ester was synthetically modified through hydrazine hydrate to acyl hydrazide which was condensed with aromatic aldehydes to afford the title N-acylhydrazones (4-17). Chemical structures of the newly synthesized compounds have been confirmed through mass, FT-IR and HNMR techniques. In vitro free radical scavenging and α-glucosidase inhibition activities of the compounds were investigated with reference to the standard ascorbic acid and acarbose, respectively. Amongst the target compounds, 13 showed the highest inhibition in DPPH scavenging assay (IC = 131.50 µM) and α-glucosidase inhibition potential (IC = 352 µg/ml). We extended our investigations to explore the mechanism of enzyme inhibition and conducted docking analysis by using Molecular Operating Environment (MOE 2016.08). A ho...

Peramivir is a potent neuraminidase (NA)
inhibitor for treatment of influenza infection by intravenous
administration. By replacing the carboxylate group in peramivir
with a phosphonate group, phosphono-peramivir (6a), the
dehydration and deoxy derivatives (7a and 8a) as well as their
corresponding monoalkyl esters are prepared from a pivotal
intermediate epoxide 12. Among these phosphonate compounds,
the dehydration derivative 7a that has a relatively rigid
cyclopentene core structure exhibits the strongest inhibitory
activity (IC50 = 0.3−4.1 nM) against several NAs of wild-type
human and avian influenza viruses (H1N1, H3N2, H5N1, and H7N9), although the phosphonate congener 6a is unexpectedly
less active than peramivir. The inferior binding affinity of 6a is attributable to the deviated orientations of its phosphonic acid and
3-pentyl groups in the NA active site as inferred from the NMR, X-ray diffraction, and molecular modeling analyses. Compound
7a is active to the oseltamivir-resistant H275Y strains of H1N1 and H5N1 viruses (IC50 = 73−86 nM). The phosphonate
monoalkyl esters (6b, 6c, 7b, 7c, 8b, and 8c) are better anti-influenza agents (EC50 = 19−89 nM) than their corresponding
phosphonic acids (EC50 = 50−343 nM) in protection of cells from the viral infection. The phosphonate monoalkyl esters are
stable in buffer solutions (pH 2.0−7.4) and rabbit serum; furthermore, the alkyl group is possibly tuned to attain the desired
pharmacokinetic properties.

5-Amino-3-(3-methyl-5-oxo-1-phenyl-2-pyrazolin-4-yl)-7-phenyl-7H-thiazolo[3,2-a]pyrimidine-6-carbonitrile was synthesized via the reaction of 4-(2-aminothiazol-4-yl)-3methyl-1-phenyl-2-pyrazolin-5-one with benzylidene malononitrile and was then transformed to related fused heterocyclic systems. The antifungal and antibacterial studies revealed in some cases excellent biocidal properties.