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33 Cards in this Set

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