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85 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Class that inhibits murein polymer crosslinking
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Beta-Lactam Antibiotics
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Acts synergisically with beta-lactams and binds the 30S ribosomal subunit
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Aminoglycosides
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Classes of Beta-lactams
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Penicillins
Cephalosporins Monobactams Carbapenems |
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Acts synergisically with beta-lactams and binds the 30S ribosomal subunit
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Aminoglycosides
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The function of beta-lactamase and three examples of inhibitors
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Beta-lactamase cleaves the active site of the beta-lactam ring.
Cavulanic acid Sulbactam Tazobactam |
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Inhibitors of metabolism
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Sulfonamides
Trimethoprim |
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Acts synergisically with beta-lactams and binds the 30S ribosomal subunit
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Aminoglycosides
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Ethambutol action
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Prevents arabinogalactan synthesis by Inhibiting arabinosyl tranferase
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Resistance conferred by mutation in arabinosyl transferase
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Five subclasses of Penicillins
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Penicillin G and V
Antistaphylococcal Penicillin Amino Penicillin Carboxy Penicillin Ureido Penicillin |
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Inhibitors of metabolism
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Sulfonamides
Trimethoprim |
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Most common adverse effect from Beta-lactam therapy and mechanism
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Hypersensitivity Reaction
Beta-lactam can react with amino groups on proteins to form hapten-carrier complex |
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Pyrazinamide action
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Converted in the cell to parazionic acid by piraziamidase
Inhibits FAS I from converting Acetyl CoA to Saturated Fatty Acid |
Resistance conferred by mutation in enzyme which converts prodrug into drug
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Inhibitors of metabolism
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Sulfonamides
Trimethoprim |
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Isonizid action
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Activated intracellularly by Catalase-peroxidase enzyme
Inhibits FAS II from linking Saturated Fatty Acids |
Resistance conferred by mutation in enzyme which converts prodrug into drug
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Inhibitors of cell wall synthesis
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B-lactams
Vancomycin |
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Ethambutol action
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Prevents arabinogalactan synthesis by Inhibiting arabinosyl tranferase
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Resistance conferred by mutation in arabinosyl transferase
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Inhibitors of protein synthesis
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Tetracyclines
Aminoglycosides Macrolides Clindamycin Chloramphenicol |
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Classes of 50S inhibitors
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Chloramphenicol
Oxazolidinones/Linezolid Lincosamines/Clindamycin Macrolides Ketolides Streptogramins |
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Inhibitors of cell membrane function
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Isoniazid
Amphotericin B |
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Binding site for 50S inhibitors
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The peptidyl transferase ring (PTR) within the peptidyl tranferase center (PTC) on 23S rRNA
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Inhibitors of nucleic acid synthesis or function
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Fluoroquinolones
Rifampin |
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Pyrazinamide action
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Converted in the cell to parazionic acid by piraziamidase
Inhibits FAS I from converting Acetyl CoA to Saturated Fatty Acid |
Resistance conferred by mutation in enzyme which converts prodrug into drug
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Mechanisms of transfer of ABX resistance: List and Define
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Transformation- Uptake and incorporation of free DNA
Conjugation- Cell-to-Cell Transfer of DNA Transduction- Transfer of DNA by Transducing Bacteriophage |
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Translation steps involving PTR
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Binding aa-tRNA, peptidyl bond formation, and translocation
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Inhibitors of Monomer Synthesis
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Fosfomycin
Fosmidomycin Cycloserine |
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Chloramphenicol mode of inhibition
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Bind in the A-site, interferes with proper positioning of aa-tRNA inhibiting peptidyl transferase
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Isonizid action
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Activated intracellularly by Catalase-peroxidase enzyme
Inhibits FAS II from linking Saturated Fatty Acids |
Resistance conferred by mutation in enzyme which converts prodrug into drug
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Cycloserine action
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Structural analogue of D-ala
Irreversably binds to Racemace and D-ala-D-ala Synthetase |
Resistance due to increases uptake of D-ala
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Oxazolidinone/Linezolid mode of inhibition
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Binds both A and P-site. Binds U2585 residue preventing conformational change required to correctly position aa-tRNA from A-site to P-site
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Inhibitors of polymerization
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Bacitracin
Vancomycin Teicoplanin |
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Lincosamine/Clindamycin mode of inhibition
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Bind both A and P-site preventing tRNA positioning in both sites inhibiting peptidyl transferase
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Bacitracin Action
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Inhibits dephosphorylation of Bactoprenol Phosphate
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Classes of 50S inhibitors
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Chloramphenicol
Oxazolidinones/Linezolid Lincosamines/Clindamycin Macrolides Ketolides Streptogramins |
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Vancomycin/Teicoplanin action
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Binds to D-ala-D-ala-NAG terminus of murein monomer preventing addition to polypeptide
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Resistance from subtitution to D-ala-D-lactate
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Macrolide/Ketolide mode of inhibition
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Bind in the exit tunnel below PCT on 23S blocking the peptide from leaving the ribosome resulting in abortion of protein synthesis.
Also binds 50S precursores preventing their synthesis. |
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Structural analogue of B-lactams
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D-ala-D-ala
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Two subgroups of Streptogramins
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Dalfopristin (Streptogramin A)
Quinupristin (Streptogramin B) Must be used synergistically to be clinically effective |
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6-ring B-lactam
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Cephalosporin
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Binding site for 50S inhibitors
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The peptidyl transferase ring (PTR) within the peptidyl tranferase center (PTC) on 23S rRNA
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Murein monomers are added to...
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NAG of growing polypeptide
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Dalfopristin (Streptogramin A) mode of inhibition
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Binds within the PTR and prevents positioning of A and P-site tRNA.
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Ethambutol action
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Inhibits arabinosyl tranferase
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Resistance conferred by mutation in arabinosyl transferase
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Translation steps involving PTR
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Binding aa-tRNA, peptidyl bond formation, and translocation
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Pyrazinamide action
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Inhibits FAS I from converting Acetyl CoA to Saturated Fatty Acid
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Resistance conferred by mutation in enzyme which converts prodrug into drug
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Quinupristin (Streptogramin B) mode of inhibition
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Binds in the exit tunnel preventing extension of the peptide chain.
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Isonizid action
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Inhibits FAS II from linking Saturated Fatty Acids
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Resistance conferred by mutation in enzyme which converts prodrug into drug
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Chloramphenicol mode of inhibition
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Bind in the A-site, interferes with proper positioning of aa-tRNA inhibiting peptidyl transferase
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Oxazolidinone/Linezolid mode of inhibition
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Binds both A and P-site. Binds U2585 residue preventing conformational change required to correctly position aa-tRNA from A-site to P-site
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What is responsible for the high selectivity of Macrolides/Ketolides
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The binding residue A2058 is not conserved from bacteria to eukaryotic or even mitochondrial rRNAs.
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Lincosamine/Clindamycin mode of inhibition
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Bind both A and P-site preventing tRNA positioning in both sites inhibiting peptidyl transferase
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Mupirocin mode of inhibition
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It mimics Isoleucyl-AMP and can bind and inactivate Isoleucine-tRNA-synthetase
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Macrolide/Ketolide mode of inhibition
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Bind in the exit tunnel below PCT on 23S blocking the peptide from leaving the ribosome resulting in abortion of protein synthesis.
Also binds 50S precursores preventing their synthesis. |
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Inhibitors of 30S subunit
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Aminoglycosides
Spectinomycin Tetracyclines |
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Two subgroups of Streptogramins
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Dalfopristin (Streptogramin A)
Quinupristin (Streptogramin B) Must be used synergistically to be clinically effective |
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Aminoglycosides mode of inhibition
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Target A-site on16S rRNA.
At low concentration-Induces misreading decreasing fidelity At high concentrations- cmpletely inhibit protein synthesis by trapping ribosomes at AUG start codon of mRNA |
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Dalfopristin (Streptogramin A) mode of inhibition
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Binds within the PTR and prevents positioning of A and P-site tRNA.
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Spectinomycin mode of inhibition.
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Binds helix34 on 16srRNA which requires conformational flexibility to translocate. Binding locks ribosome in place.
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Quinupristin (Streptogramin B) mode of inhibition
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Binds in the exit tunnel preventing extension of the peptide chain.
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Tetracycline mode of inhibition
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Binds reversably to 16S rRNA in the A-Site competing with aa-tRNA. aa-tRNA can not enter the A-Site while occupied by tetracycline.
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What is responsible for the high selectivity of Macrolides/Ketolides
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The binding residue A2058 is not conserved from bacteria to eukaryotic or even mitochondrial rRNAs.
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Mupirocin mode of inhibition
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It mimics Isoleucyl-AMP and can bind and inactivate Isoleucine-tRNA-synthetase
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Inhibitors of 30S subunit
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Aminoglycosides
Spectinomycin Tetracyclines |
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Classes of Topoisomerase (DNA synthesis) inhibitors
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Aminocoumarines
Quinolones |
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Aminoglycosides mode of inhibition
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Target A-site on16S rRNA.
At low concentration-Induces misreading decreasing fidelity At high concentrations- cmpletely inhibit protein synthesis by trapping ribosomes at AUG start codon of mRNA |
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Aminocoumarin mode of inhibition
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Binds B-subunit (GyrB) of DNA Gyrase (Type II topoisomerase) by competing with ATP
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Spectinomycin mode of inhibition.
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Binds helix34 on 16srRNA which requires conformational flexibility to translocate. Binding locks ribosome in place.
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Quinolone mode of inhibition
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Binds to GyrA subunit and cleaved end of DNA molecule stabilizing the complex preventing the second DNA strand to pass through.
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Tetracycline mode of inhibition
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Binds reversably to 16S rRNA in the A-Site competing with aa-tRNA. aa-tRNA can not enter the A-Site while occupied by tetracycline.
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Inhibitor of RNA Synthesis
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Rifamycin/Rifampin
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Classes of Topoisomerase (DNA synthesis) inhibitors
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Aminocoumarines
Quinolones |
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Rifamycin/Rifampin Mode of inhibition
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Binds B-subunit of RNA polymerase preventing trancscription initiation and forming a stable complex between the RNA pol and DNA strand
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Aminocoumarin mode of inhibition
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Binds B-subunit (GyrB) of DNA Gyrase (Type II topoisomerase) by competing with ATP
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Essential Metabolite Inhibitors
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Sulfonamides
Trimethoprim/ Pyrimethamine/ Methotrexate |
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Quinolone mode of inhibition
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Binds to GyrA subunit and cleaved end of DNA molecule stabilizing the complex preventing the second DNA strand to pass through.
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Sulfonamide mode of inhibition
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A structural analogue of PABA, it competitively inhibits Dihydropteorate Synthetase
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Inhibitor of RNA Synthesis
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Rifamycin/Rifampin
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Trimethoprim/ Pyrimethamine/ Methotrexate mode of inhibition
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A structural analogue of folate, it competitively inhibits Dihydrofolate Reductase
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Rifamycin/Rifampin Mode of inhibition
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Binds B-subunit of RNA polymerase preventing trancscription initiation and forming a stable complex between the RNA pol and DNA strand
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Antimycobacterial Drugs
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Rifamycin/Rifampin
Streptogramin/Streptomycin Ethambutol Pyrazinamide Isoniazid (INH) |
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Essential Metabolite Inhibitors
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Sulfonamides
Trimethoprim/ Pyrimethamine/ Methotrexate |
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Tetrahydrofolate (THF) is a precursor for...
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Purines, Thymine, Methionine
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Sulfonamide mode of inhibition
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A structural analogue of PABA, it competitively inhibits Dihydropteorate Synthetase
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Trimethoprim/ Pyrimethamine/ Methotrexate mode of inhibition
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A structural analogue of folate, it competitively inhibits Dihydrofolate Reductase
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Antimycobacterial Drugs
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Rifamycin/Rifampin
Streptogramin/Streptomycin Ethambutol Pyrazinamide Isoniazid (INH) |
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Tetrahydrofolate (THF) is a precursor for...
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Purines, Thymine, Methionine
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