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Medicinal Chemistry Unit 01 Syllabus -
(A) Antibiotics - Historical background, nomenclature, stereochemistry, structure-activity relationship, chemical degradation, classification and important product of these classes -
(01) Beta-lactam antibiotics - Penicillin, Cephalosporins, beta-lactamase inhibitors, Monobactam
(02) Aminoglycosides - Streptomycin, Neomycin, Kanamycin
(03) Tetracycline - tetracycline, Oxytetracycline, Chlortetracycline, Minocycline, Doxycycline
Introduction to Antibiotics
Antibiotics are chemical compounds used to kill or inhibit the growth of bacteria. Strictly speaking, antibiotics are a subgroup of organic anti-infective agents that are derived from bacteria or moulds that are toxic to other bacteria. The term antibiotic may be used interchangeably with the term antibacterial.
History of antibiotics
Penicillin was the first antibiotic used successfully in treating bacterial infections. Sir Alexander Fleming first discovered it in 1928, but its potential for treatment against infections wasn’t recognised until over a decade later when Ernst B Chain, Sir Howard Florey and Norman Heatley produced enough purified penicillin to treat patients with. By the 1950s, a large number of antibiotics were being discovered and manufactured for the treatment of diseases caused by infecting bacteria. Over the last 50 years, antibiotics have transformed the patterns of disease and death.
Classification of antibiotics
Antibiotics can be classified in several ways. The most common method classifies them according to their chemical structure as antibiotics sharing the same or similar chemical structure will generally show similar patterns of antibacterial activity, effectiveness, toxicity and allergic potential.
1. B-lactam antibiotics inhibit bacterial cell wall synthesis. They include:
Penicillins, Penicillin G, Amoxicillin, Flucloxacillin
CephalosporinsCefoxitin, Cefotaxime, Ceftriaxone, Carbapenem
2. Macrolides inhibit bacterial protein synthesis.
ErythromycinAzithromycin Clarithromycin
3. Tetracyclines inhibit bacterial protein synthesis.
Tetracycline Minocycline DoxycyclineLymecycline
4. Fluoroquinolones inhibit bacterial DNA synthesis.
Norfloxacin, Ciprofloxacin, Enoxacin, Ofloxacin
5. Sulphonamides block bacterial cell metabolism by inhibiting enzymes.
Trimethoprim + sulphamethoxazole
6. Aminoglycosides inhibit bacterial protein synthesis.
Gentamicin, Amikacin
7. Imidazole antibiotics inhibit bacterial DNA synthesis.
Metronidazole
8. The following drugs inhibit bacterial protein synthesis.
Fusidic acid, Mupirocin
Uses of antibiotics
Antibiotics only work against infections caused by bacteria. Bacterial infections are much less common than viral infections. Most coughs and colds are of viral origin so antibiotics should not be prescribed for these. Antibiotics should only used when absolutely necessary, because:
1. There is increasing resistance of bacteria to treatment.
2. Resistant bacteria are selected out by the use of antibiotics.
3. Antibiotics may have serious adverse effects in some people.
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