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Hint
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Answer
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Antibiotics - Cell wall biosynthesis inhibitors
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Bactoprenol dephosphorylation inhibitor (prevents recycling) Made through Lipid I and II intermediates ad bactoprenol carrier
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Bacitracin
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D-alanyl-D-alanine synthase +ligase inhibitor
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D-Cycloserine
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mimics D-ala-D-ala to inhibit transpeptidase action (beta-lactam ring)
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Penicillin
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Binds D-ala-D-ala to modify lipid 2 and inhibit transglycosylase action
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Vancomycin
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Ribosome Targeters
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Aminoglycoside binds A site on 16s rRNA on 30s (bacteriostatic)
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Tetracycline
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Aminoglycoside binds 30s + nephrotoxic + ototoxic
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Streptomycin
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Less toxic aminoglycoside
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Gentamycin
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Inhibits elongation factor G
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Spectinomycin
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Binds co-operativley on A site with Streptomycin
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Paromomycin
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50s targeters
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Macrolide, binds E site via 23s rRNA on 50S overlaps P site to compete vs peptidyl transferase inhibitors (lincomycin)
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Erythromycin
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binds A site to inhibit peptidyl transferase on 50s (overlaps binding site with clindamycin)
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Chloramphenicol
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Prevents translocation via GTPase+efG inhibition
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Fusidic acid
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blocks translocation at 50s (is synergistic combination)
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Synercid
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Protein Synthesis inhibitors
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Inhibits GyrB (topo II ATP binding portion) aminocoumarin
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Novobiocin
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Aminocoumarin, inhibits GyrB
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Coumermycin
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Chloroquine by product, inhibits GyrB
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Nalidixic acid
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Flouroquinolone, inhibits DNA Gyrase
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Ciprofloxacin
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Flouroquinolone, inhibits DNA gyrase
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Levofloxacin
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Inhibits DNA-dependent RNA Polymerase, binds exit tunnel to prevent elongation
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Rifampin
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DNA Binding molecules
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Intercalates with bases to stretch backbone
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Daunomycin
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metal chelating glycoprotein that intercalates minor groove
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Bleomycin
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Alkylates DNA (forms G-G crosslinks between strands)
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Mitomycin C
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Anti-metabolites
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Inhibits Dihydropteroate Synthase (sulfonamide)
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Sulfamethazole
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Inhibits Dihydrofolate reductase (diaminopyrimidines)
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Trimethoprim
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Formulation of the above
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Co-trimoxazole
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Membrane targetting drugs
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Forms potassium uniport
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Valinomycin
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Forms transmembrane ion channel upon dimerisation
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Gramicidin A
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Potassium antiporter
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Nigericin
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Sodium antiporter
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Monesin
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Binds Lipid A of LPS to form leaky envelope (polymyxin E)
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Colistin
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Anti-fungals
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Forms pores via ergosterol binding
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Amphotericin B
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Forms pores via ergosterol binding
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Nystatin
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Triazole that inhibits ergosterol synthesis
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Fluconazole
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Imidazole that inhibits ergosterol synthesis
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Miconazole
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Anti-protozoal
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Arsenic pro-drug that inhibits ATP synthesis via TCA cycle, PFK, PDH, Pyruvate kinase inhibition (accumulates in Trypanosomes)
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Melarsoprol
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Inhibits reoxidation of NADH and ATP synthesis
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Suramin
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Leishmaniasis (has ergosterol in membrane)
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Inhibits Topo I and ATP synthesis
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Sodium Stibogluconate
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Anti-malarials
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Inhibits haemozin formation (store of toxic haem from Hb digestion by parasite)
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Chloroquine
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Activated by iron in haem to form free radicals
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Artemisinin
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DHFS inhibitor
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Sulfadoxin
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DHFR inhibitor
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Pyrimethamine
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DHFR inhibitor pro-drug
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Proguanil
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Hydroxynapthoquinone that mimics ubiquinone to inhibit etc
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Atavoquone
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Tetracycline Analogue
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Doxycycline
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Chloramphenicol Analogue
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Clindamycin
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Anti-herpes
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Purine analogue activated by viral thymidine kinase
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Acyclovir
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