Cology II: medchem

synthetic sulfonamide antibiotic - synthetic agent

block folic acid synthesis

quinolone antibiotics- synthetic agent

inhibits dna gyrase/topoisomerase in dna replication

aminoglycoside

inhibit protein synthesis, contain 1,3-diaminoinositol pharmacophore

topical, ointment, IV

trimethoprim- synthetic agent

inhibit dihydrofolate reductase in thymidine synthesis pathway

penicillin

prokaryote bacteria with cell wall, rigid and complex petidoglycan in polymeric sheets

fused b lactam with thiazolidine ring strained and reactive

cephalosporin

b lactam annealed to 6 member dihydrothiazine ring

carbapenem/monobactam

s removed from ring, moved to functionalized group on C3

-monobactam: ring fused to b lactam removed

macrolide/tetracycline

macrolide: 14 membered ring, lactone cyclic ester

tetracycline: tricarbonyl, highly enolized

nitroaryl compounds

quinolone antimalarials

block detoxification, induces toxicity in parasite

artemisinins

formation of endoperoxide (O-O-) from di/trioxanes

benzimidazoles (antihelmintics)

inhibit fumarate reductase and enzyme involved in recycling of NAD)H) in glycolysis, binds tubulin and prevent its polymerization to microtubules

pyrethroids

toxins to parasite nerve membrane NA channels

polyene membrane disruptors

ergosterol biosynthesis inhibitors

14 a demethylase, converts methyl moiety to alcohol, aldehyde, carboxylic acid

release HCOOH

CYP51 target of azole antifungals

azole antifungals

demethylase used by mammals and fungi, azoles ar epotentent cyp3a4 inhibitors and interfere with p-glycoprotein

squalene epoxidase inhibitors

allylamines: naftifine/terbinafine; butenafine: phenyl ring

echinocandins (cell wall synthesis inhibitors)

fungi have cell wall that is absent in mammals

-lipopeptides block cell wall formation through inhibiting B-1-3-glucan synthase

anti-herpesvirus agents + gunanin nucleoside analogs (non retroviral)

acyclovir, penciclovir, ganciclovir

influenza antivirals (non retroviral)

m2 protein inhibitors: amantadine, rimantadine

neuraminidase inhibitors: oseltamivir, zanamivir, peramivir (non retroviral)

foscarnet (non retroviral drug)

new chlorohexidine drugs (non retroviral)

letermovir: UL56 terminase inhibitor

maribavir: UL97 kinase virale inhibitor

xofluza (Baloxavir marboxil)

inhibits influenza polymerase acidic endonuclease, prevents viral replication

drugs targeting HCV and covid (non retro viral)

antiretroviral drugs: entry inhibitors

Fostemavir, maraviroc

antiretroviral: nucleoside reverse transcriptase inhibitors

acyclic nucleosides: acyclcovir, ganciclovir, cidofovir(antiretroviral)

acyclic nucleosides (antiretroviral)

adefovir, tenofovir disoproxil, famciclovir

acyclic nucleotide prodrugs (antiretroviral): adefovir

acyclic nucleotide prodrugs (antiretroviral): tenofovir

conventional nucleoside analogs

ribavirin: triphosphate inhibits viral rna polymerase and block nucleic acid synthesis

idoxuridine: triphosphate inhibits viral dna polymerase and terminate dna synthesis via disabled base pairing

halides and 2, 3-dihydroxy: both can disrupt viral dna replication

nucleoside RT and dna polymerase inhibitors (antiretroviral)

into viral dna=chain termination

protease inhibitors (antiretroviral)

capsid inhibitor (antiretroviral)

integrase inhibitors (antiretrovial)