Scribd Logo
Upload

Welcome to Scribd!

    • 7 views

    SAR of Cephalosporin

    Uploaded by

    Muhammad Sadiq
    Cephalosporin

    Copyright:

    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd

    SAR of Cephalosporin

    Uploaded by

    Muhammad Sadiq
    7 views3 pages
    Cephalosporin

    Original Title

    SAR of cephalosporin

    Copyright

    © © All Rights Reserved

    Available Formats

    DOCX, PDF, TXT or read online from Scribd

    Did you find this document useful?

    Is this content inappropriate?

    Cephalosporin

    Copyright:

    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    7 views3 pages

    SAR of Cephalosporin

    Uploaded by

    Muhammad Sadiq
    Cephalosporin

    Copyright:

    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    You are on page 1of 3

    To detail 20 structure-activity relationships (SAR) for cephalosporins, we need to consider various

    aspects of their chemical structure and how these aspects influence their biological activity. Here’s a
    comprehensive list:

    1. **Beta-Lactam Ring Integrity**: Essential for activity. Modification can lead to loss of antimicrobial
    efficacy.

    2. **Dihydrothiazine Ring**: The presence of this ring is crucial for maintaining beta-lactamase stability
    and activity.

    3. **R1 Side Chain Variations**: Changes in the R1 side chain affect beta-lactamase resistance and
    spectrum of activity. For example, electron-withdrawing groups may enhance stability against certain
    beta-lactamases.

    4. **R2 Side Chain Variations**: Alterations here can affect antibacterial activity, spectrum, and
    pharmacokinetics. For instance, bulky groups can increase resistance to beta-lactamases.

    5. **Cephalosporin C vs. 7-ACA**: Cephalosporin C has an additional side chain at position 3 compared
    to 7-ACA, which can enhance its activity and spectrum.

    6. **C-3 Side Chain**: The presence and type of the C-3 side chain (e.g., acetoxymethyl) affect the
    drug’s stability and activity against Gram-negative bacteria.

    7. **C-7 Side Chain**: Changes here can influence the drug’s spectrum of activity and resistance to
    beta-lactamases. For example, the addition of methoxy groups can improve activity against certain
    strains.

    8. **C-6 Alpha-Methyl Group**: This modification can enhance resistance to beta-lactamases and
    improve stability.
    9. **C-7 Amino Group**: Alterations can affect antimicrobial activity and susceptibility to hydrolysis by
    beta-lactamases.

    10. **Presence of a Carbonyl Group**: The position and presence of carbonyl groups can influence the
    stability and activity of cephalosporins.

    11. **Sulfur Atom in the Dihydrothiazine Ring**: Essential for maintaining activity and resistance to
    beta-lactamases.

    12. **Oxime Side Chain**: Modifications to this side chain can improve resistance to beta-lactamase
    hydrolysis and enhance antibacterial activity.

    13. **Aryl Substituents on the R1 Side Chain**: These can influence pharmacokinetic properties and
    activity against specific bacteria.

    14. **Piperazine Ring Substitutions**: Substitutions on a piperazine ring (when present) can affect the
    drug’s activity spectrum and resistance profile.

    15. **Hydroxyl Group at C-3**: The presence of hydroxyl groups can affect the solubility and stability of
    the cephalosporin.

    16. **N-Methyl Group on the Beta-Lactam Ring**: This can influence the drug's ability to interact with
    bacterial penicillin-binding proteins.

    17. **Amino Acid Substituents**: Incorporation of amino acids into the structure can enhance activity
    against specific bacterial strains.

    18. **Ethyl Ester Groups**: These groups can impact the pharmacokinetic properties, including
    absorption and distribution.
    19. **Fluoro-Substituents**: Fluorine atoms can enhance the drug’s resistance to metabolic
    degradation and increase activity against specific bacteria.

    20. **Beta-Lactam Ring Substitution Patterns**: Specific substitution patterns can optimize the
    cephalosporin’s ability to bind to bacterial penicillin-binding proteins and overcome resistance
    mechanisms.

    Each modification impacts the drug’s interaction with bacterial targets, its pharmacokinetics, and its
    overall effectiveness against different bacterial strains. Understanding these relationships helps in
    designing more effective cephalosporin antibiotics.

    You might also like