抗生素(英文精品) Antibiotics(51p)讲解说明.pptVIP

Chapter 8 Antibiotics;Antibiotics as disturber with the biosynthesis of protein ;Tetracycline Antibiotics ;Tetracyclines are produced by actinomyces (放线菌), which have broad-antibacterial spectrum. The basic skeleton of tetracyclines is naphthacene ring. Tetracyclines differing from each other chemically only by substituent variation at positions 5,6 and 7.;Tetracycline;Stability under acid condition;Formation of 4-Epitetracycline;Stability under base condition;Formation of metal chelates;Aminoglycoside Antibiotics ;The aminoglycoside class of antibiotics contains a pharmacophoric 1,3-diaminoinositol (1,3-二氨基肌醇) derivatives;Chemistry ;Caution !;Chemistry;Spectrum of activity ;Mechanism of Action ;;Toxicity;Streptomycin(链霉素) ;;;Clinical Use ;Macrolide Antibiotics;Macrolide Antibiotics ;Mechanism of action;;Erythromycin (红霉素）;Erythromycin;Extremely unstable under acid condition;Simply modification of erythromycin-Ester Pro-drug;Strategy for erythromycin modification;;Erythromycin derivatives;Telithromycin;In addition to the C-3 ketone, telithromycin has an aromatic N-substituted carbamate extension at position C-11 and C-12. This ring has an imidazo-pyridyl group attachment. Telithromycin possesses a 6-OCH3 group (like clarithromycin), avoiding internal kemiketalization with the 3-keto function and giving the ketolide molecule excellent acid stability. The ketolides are very active against respiratory pathogens, including erythromycin-resistant strains ;Chloramphenicol Antibiotics;Chloramphenicol (氯霉素 );A molecule, with two chiral centers, has four isomers (diastereomers). ;;Chemical properties;Chloramphenicol is bacteriostatic by inhibition of protein biosynthesis. Its toxicities prevent Chloramphenicol from being more widely used. The major adverse effect of chloramphenicol is a risk of fatal irreversible aplastic anemia that occurs after therapy and does not appear to be related to dose or administration route. Reversible bone marrow suppression and several oth