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33 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Sulfonamides
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inhibit dihydropteroate synthase, prevents incorporation of PABA into dihydropteroic acid
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prevent folic acid synthesis
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Trimethroprim
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competively inhibit DHFR (Dihydrofolate reductase)
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for bac, but can inhibit human at hgih con
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Quinolones
(cipro, levo, gati, moxi, trova) |
DNA gyrase (gyrA): GNev
Topoisomerase 4 (parC): (+) |
both enz important for DNA replication
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Aminoglycosides (gent, tob, strepto, amikacin, kanamycin)
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binds to 30S, fix 30S-50S at mRNA
incorporate incorrect aa |
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Tetracycline
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binds 30S, prevent access to aminoacetyl-tRNA to "A" site
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Chloramphenicol
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bind reversibly to 50S (peptidyl transferase enzy), prevent peptide bond formation, inhibit elongation
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Macrolides (Azith, Clari, Erythromycin)
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bind 50S, inhibit translocation process of PS
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Lincosamides (clindamycin, lincomycin)
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binds to 50S, inhibit PS
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Quinupristin/Dalfopristin
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binds to 50S, prevent peptide elongation and early termination of PS
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Oxazolidinone (Linezolid, Eperezolid)
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binds 23r rRNA of 50S, prevent formation of 70S initiation complex
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Vancomycin
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binds to D-ala-D-ala terminus, inhibit the polymerization and chain elongation, inhibit cell wall synthesis
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Isoniazid
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inhibit FAS2 enzy, inhibit biosynthesis of mycolic acids (imp component of mycobacterial cell wall)
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Rifampin
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inhibit DNA-dependent RNA polymerase of mycobacterium
or viral ... if at high con |
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Ethambutol
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blocks arabinosyl transferase enzy (essential for cell wall biosynthesis), disrupt cell wall and cause cell leakage
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Pyrazinamide
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inhibits FAS1, PZase/nicotinamidase (PSA2); interfere the mycolic acid biosynthesis pw
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R207910 (new TB drug)
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blocks membrane ATP synthase- enzyme that makes ATP
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Dapsone
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tx of Leprosy
inhibit bacterial folate biosynthesis pw |
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Echinocandins (caspofungin-Candidas; Micafungin)
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inhibit B(1,3)-D-glucan synthase enzyme
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Nikkomycin Z, Nikkomycin X
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chitin synthase inhibitors
structural analogs of UDP-N-acetylglucosamine |
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Azoles (itraconazole, fluconazole, voriconazole, posaconazole, ravuconazole)
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inhibits CYP450 enzyme in 14alpha-demethylation process (abnormal accumulation of lanosterol and other precursors)
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Imidazoles (clotrimazole, miconazole, ketoconazole, econazole, butoconazole)
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inhibit sterol 14 alpha-demethylase enz (a P450 dependent enzyme sys)
impairs biosynthesis of ergosterol in cytoplasmic mem lead to acumulation of 14alpha methylsterols |
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Allylamines
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inhibit ergosterol synthesis
(inhibits squalene epoxide: early stage of ergosterol synthesis) |
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Terbinafine (lamisil)
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onychomycosis (nail infection)
highly lipophilic, accumulate in skin, nails, Fatty tissues |
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Naftifine
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onychomycosis (nail infection)
highly lipophilic, accumulate in skin, nails, Fatty tissues |
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Phenylmorphine (amorolfine- Loceryl)
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inhibit ergosterol synthesis
blocsk 14-reduction & 7.8 isomerisation) formulated as nail lacquer-water insoluble film on nail that last for extended duration |
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Polyenes (nystain, amphotericin B)
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bind to fungal sterols, disrupt membrane structure/integrity
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Group 1 Polyenes
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cell leakage and lysis at same concentration
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group 2 polyenes
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cell leakage: low con
cell lysis: high con |
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amphotericin B
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binds ergosterol, disrupt osmotic integrity, form pore, leakage of cell content, cell die
affinity: ergosterol> cholesterol |
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taxol
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bind to microtubule and stabilize them, arrests cells in mitosis
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Colchicine
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alkaloid from meadow saffron
bind irreversibly to beta-tubulin monomer, prevent its polymerisation, and destabilizes polymers |
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colcemide, vinblastine, vincristine, nocodazole
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binds to monomers, prevent polymerisation of tubulin
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Griseofulvin
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inhibitors of microtubule assembly;
disrupt mitotic spindle by interacting with the polymerized microtubules (binding sites # vinca and taxol); inhibit fungal mitosis--> formation of nucleated cells |
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