From Walsh, Christopher. Antibiotics: Actions, Origins, Resistance.Washington, D.C.: ASM Press,2003
........................................Introd.......Resist.
Sulfonamides.....................1930s........1940s
Penicillin.......... .................1943.........1946
Streptomycin......................1943.........1948
Bacitracin...........................1945.........1953
Chloramphenicol ............... 1947.........1959
Cephalosporin .................. 1960s...late1960s
Neomycin...........................1949 ........1950
Tetracycline ......................1948.........1953
Erythromycin.....................1952.........1988
Vancomycin.......................1956.........1988
Kanamycin.........................1957.........1966
Methicillin..........................1960.........1961
Ampicillin...........................1961.........1973
Gentamicin.........................1963.........1969
Carbenicillin.......................1964.........1974
Clindamycin.......................1969.........1970
Amoxicillin.........................1972.........1975
Piperacillin.........................1980.........1981
Augmentin ........................1984........ 1984
Aztreonam ........................1984........ 1985
Imipenem..........................1985.........1985
Ciprofloxacin.....................1987.........1987
Quinupristin-Dalfopristin....1999.........2000
Linezolid............................2000.........2002
1. Inhibition of cell wall synthesis
2. Interference with membrane integrity
3. Inhibition of nucleic acid synthesis
4. Inhibition of protein synthesis
5. Inhibition of synthesis of essential
small molecules
6. Miscellaneous (or unknown) effects
Inhibition of Cell Wall Synthesis
Drugs that Inhibit Cell Wall Biosynthetic Enzymes
Drugs that Bind to Carrier Molecules
Drugs that Combine with Cell Wall Precursors
Drugs that Inhibit Enzymatic Polymerization and Attachment of New
Peptidoglycan to Cell Wall (β-Lactams)
Interference with Cytoplasmic Membrane Integrity
Drugs that Disorganize the Cytoplasmic Membrane
Drugs that Produce Pores in Membranes
Inhibition of Nucleic Acid Synthesis
Inhibitors of DNA Replication
Inhibitors of RNA Polymerase: Rifamycins (Rifampin and Rifaximin)
Inhibition of Ribosome Function and Protein Synthesis
Inhibitors of 30S Ribosomal Subunits
Inhibitors of 50S Ribosomal Subunits
Inhibition of Synthesis of Essential Small Molecules
Inhibitors of Dihydropteroate Synthetase
Inhibitors of Dihydrofolate Reductase
Antimycobacterial Agents
Inhibition of Cell Wall Synthesis
......Isoniazid (Isonicotinic Acid Hydrazide, INH)
......Cycloserine
......Ethambutol
Interference with Cytoplasmic Membrane Function: Pyrazinamide
Inhibition of Nucleic Acid Synthesis
…Rifamycins: Rifampin, Rifabutin,
and Rifapentine
…Fluoroquinolones as Antimycobacterial Agents
Inhibition of Protein Synthesis
Aminoglycosides: Streptomycin and Amikacin
........................................Introd.......Resist.
Sulfonamides.....................1930s........1940s
Penicillin.......... .................1943.........1946
Streptomycin......................1943.........1948
Bacitracin...........................1945.........1953
Chloramphenicol ............... 1947.........1959
Cephalosporin .................. 1960s...late1960s
Neomycin...........................1949 ........1950
Tetracycline ......................1948.........1953
Erythromycin.....................1952.........1988
Vancomycin.......................1956.........1988
Kanamycin.........................1957.........1966
Methicillin..........................1960.........1961
Ampicillin...........................1961.........1973
Gentamicin.........................1963.........1969
Carbenicillin.......................1964.........1974
Clindamycin.......................1969.........1970
Amoxicillin.........................1972.........1975
Piperacillin.........................1980.........1981
Augmentin ........................1984........ 1984
Aztreonam ........................1984........ 1985
Imipenem..........................1985.........1985
Ciprofloxacin.....................1987.........1987
Quinupristin-Dalfopristin....1999.........2000
Linezolid............................2000.........2002
The Antimicrobial Agents are divided by mechanisms of action into six major categories
1. Inhibition of cell wall synthesis
2. Interference with membrane integrity
3. Inhibition of nucleic acid synthesis
4. Inhibition of protein synthesis
5. Inhibition of synthesis of essential
small molecules
6. Miscellaneous (or unknown) effects
Mechanisms of Action
Inhibition of Cell Wall Synthesis
Drugs that Inhibit Cell Wall Biosynthetic Enzymes
Drugs that Bind to Carrier Molecules
Drugs that Combine with Cell Wall Precursors
Drugs that Inhibit Enzymatic Polymerization and Attachment of New
Peptidoglycan to Cell Wall (β-Lactams)
Interference with Cytoplasmic Membrane Integrity
Drugs that Disorganize the Cytoplasmic Membrane
Drugs that Produce Pores in Membranes
Inhibition of Nucleic Acid Synthesis
Inhibitors of DNA Replication
Inhibitors of RNA Polymerase: Rifamycins (Rifampin and Rifaximin)
Inhibition of Ribosome Function and Protein Synthesis
Inhibitors of 30S Ribosomal Subunits
Inhibitors of 50S Ribosomal Subunits
Inhibition of Synthesis of Essential Small Molecules
Inhibitors of Dihydropteroate Synthetase
Inhibitors of Dihydrofolate Reductase
Antimycobacterial Agents
Inhibition of Cell Wall Synthesis
......Isoniazid (Isonicotinic Acid Hydrazide, INH)
......Cycloserine
......Ethambutol
Interference with Cytoplasmic Membrane Function: Pyrazinamide
Inhibition of Nucleic Acid Synthesis
…Rifamycins: Rifampin, Rifabutin,
and Rifapentine
…Fluoroquinolones as Antimycobacterial Agents
Inhibition of Protein Synthesis
Aminoglycosides: Streptomycin and Amikacin
