Medicinal Chemistry

(Jacob Rumans) #1

  1. Bacterial cell wall targets
    Penicillins (bactericidal; inhibit cell wall crosslinking)
    e.g., benzylpenicillin, phenoyxmethylpenicillin, ampicillin, amoxicillin, flu-
    cloxacillin, methicillin, piperacillin
    Cephalosporins (bactericidal; inhibit cell wall crosslinking)
    e.g., cefaclor, cefalexin, cefradine, cefuroxime, cefazolin, cefotaxime, ceftriaxone,
    cefoxitin, cefsulodin, ceftazidime, ceftizoxime
    Monobactams (bactericidal,β-lactam-like activity)
    e.g., aztreonam
    Carbapenems (bactericidal,β-lactam-like activity)
    e.g., imipenem
    Bacitracin (bactericidal; interrupts mucopeptide synthesis)
    Vancomycin (bactericidal; interrupts mucopeptide synthesis)
    Cycloserine (bactericidal; interrupts synthesis of cell wall peptides)

  2. Bacterial cell membrane targets
    Polymyxins (bactericidal; disrupt bacterial membrane structural integrity)

  3. Bacterial protein synthesis
    Chloramphenicol (bacteriostatic; interrupts protein synthesis at the ribosome)
    Macrolides (bacteriostatic; interrupt protein synthesis at the 50S ribosome subunit)
    e.g., erythromycin, azithromycin, clarithromycin
    Lincomycins (bacteriostatic; interrupt protein synthesis at the 50S subunit)
    Aminoglycosides (bactericidal; interrupt protein synthesis at the 30S subunit)
    e.g., gentamicin, amikacin, kanamycin, neomycin, tobramycin
    Tetracyclines (bacteriostatic; interrupt protein synthesis at the 30S subunit)
    e.g., tetracycline, doxycycline, minocycline


EXOGENOUS PATHOGENS AND TOXINS 561

Figure 9.3 Targets for antibacterial drugs. The various classes of antibacterial drugs exert their
effects at one of the four fundamental structural components of bacteria. Each of these compo-
nents is vulnerable to drug attack. Penicillin, for example, attacks at the level of the cell wall;
chloramphenicol, however, works at the level of bacterial protein synthesis.

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