Скачать или смотреть Topic (15) Tetracycline Antibiotics (Part 03) = Structure Activity Relationship of Tetracycline

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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

Structure-activity relationship
1. Tetracyclines are composed of a rigid skeleton of 4 fused rings.
2. The rings structure of tetracyclines is divided into an upper modifiable region and a lower nonmodifiable region
3. An active tetracycline requires a C10 phenol as well as a C11-C12 keto-enol substructure in conjugation with a 12a-OH group and a C1-C3 diketo substructure.
4. Removal of the dimethylamine group at C4 reduces antibacterial activity. Replacement of the carboxyl-amine group at C2 results in reduced antibacterial activity but it is possible to add substituents to the amide nitrogen to get more soluble analogs like the prodrug lymecycline.
5. The simplest tetracycline with measurable antibacterial activity is 6-deoxy-6-demethyltetracycline and its structure is often considered to be the minimum pharmacophore for the tetracycle class of antibiotics.
6. C5-C9 can be modified to make derivatives with varying antibacterial activity

Uses
1. Various gram-positive and gram-negative bacterial infections, including vibrio infections
2. Drug of choice - rickettsiae
3. Treat gastric and duodenal ulcer disease caused by Helicobacter pylori
4. Most chlamydial infections, including sexually transmitted infections
5. In combination with other antibiotics – plague, tularemia, and brucellosis
6. No longer recommended for the treatment of gonococcal disease because of resistance.
7. Prophylaxis of protozoal infections

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