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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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Competitive inhibitor of DNA polymerase
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Ganciclovir
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Pyramidine analogue - doesn't need viral kinase
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Trifuridine
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Pyramidine analogue - needs viral kinase
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Idoxuridine
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Cytosine analogue vs CMV
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Cidofovir
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DNA pol inhibitor, pyrophosphate analogue
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Foscarnet
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Anti-HIV
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Gp41 analogue - fusion inhibitor
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Enfuvirtide
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Reverse transcriptase inhibitor
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Nevirapine
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Thymidine analogue chain terminator
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Azidothymidine
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Protease inhibtor
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Saquinavir
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Protease inhibitor
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Ritonavir
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vDNA integrase inhibitor
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Ratelgravir
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CCR5/CXCR4 antagonist
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Maraviroc
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Anti-influenza (-ve ss RNA)
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Inhibits M2 and HA to prevent fusion
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Amantadine
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Guanine analogue which inhibits end capping and vRNAPol
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Ribavirin
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Cytidine Analogue to inhibit RdRP
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Molnupiravir
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Sialic Acid analogue to inhibit NA
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Zonamivir
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Sialic Acid analogue, pro-drug
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Oseltamivir
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Anti-Neoplastic Drugs
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Alkylating agent, phosphoramide mustard (can't cross BBB)
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Cyclophosphamide
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Alkylating agent, melanin precursor analgoue
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Melphalan
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Alkylating and Carbamoylating agents (can cross BBB)
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Nitrosourea
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IV Nitrosourea
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Carmustine
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Oral Nitrosourea
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Lomustine
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Platinum based inhibitor of DNA Pol binding
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Cisplatin
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Aziridine antibiotic, alkylates DNA
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Mitomycin C
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Intercalating Anthracycline (Produces ROS)
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Doxorubicin
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Intercalating Anthracycline (Produces ROS)
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Actinomycin D
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Intercalating Anthracycline, no ROS production
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Mitoxantrone
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DHFR Inhibitor
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Methotrexate
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Pyrimidine analogue (also inhibits folate synthesis)
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FlouroUracil
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Drug to preserve some folate synthesis (formyl derivative)
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Leucovorin
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Topo I inhibitor (+camptothecin)
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Topotecan
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Topo II Inhibitor (Mitoxantrone, anthracyclines, epipodophyllotoxin)
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Etoposide
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Vinca alkaloid inhibitor of tublin polymerisation
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Vinblastine
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Vinca alkaloid
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Vincristine
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Prevents remodelling of microtubules
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Taxol
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ER Antagonist
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Tamoxifen
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Aromatase Inhibitor (inhibits Oestrogen Synthesis)
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Anastrazole
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Testosterone competitor
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Flutamide
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GnRHR Agonist to increase and inhibit testosterone synthesis
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Goserelin
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Glucocorticoid Agonist to repress lymphocyte growth
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Prednisone
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EGFR (HER2) inhibitor
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Trastuzumab
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EGFR Inhibitor vs colorectal
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Cetuximab
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VEGF Inhibitor vs angiogenesis
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Bevacizumab
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BCR-Abl Inhibitor (TyrK)
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Imatinib
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EGFR TyrK Inhibitor
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Erlotinib
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EGFR TyrK Inhibitor
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Gefitinib
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