医学精品课件之抗生素.ppt

*The synthetic routes of semi-synthetic penicillins 6-Aminopeciliianic Aicd,6-APA Penicillin G Typical drugs 1* Benzylpenicillin (青霉素G，苄青霉素） 青霉素G由青霉菌发酵得到，临床上已经用了半个多世纪，主要用其钠盐、钾盐。其特点是抗菌作用强，用于各种球菌和革兰氏阳性菌引起的全身或局部的感染。 其缺点是化学性质不稳定，易水解，只能注射给药。 2.*Ampicilin Sodium(氨苄西林) 第一个用于临床的广谱口服青霉素,适用于革兰氏阳性球菌、杆菌、厌氧菌等所引起的呼吸道、尿道、肠道等感染。 3.*Amoxicilin Sodium(阿莫西林，羟氨苄青霉素) 口服青霉素,与氨苄西林具有相同的抗菌谱，口服吸收好，血药浓度高，除对革兰氏阳性有较高活性外，对淋球菌、流感杆菌、百日咳杆菌、大肠杆菌等也有较强作用，但使用后易产生耐药性，临床上主要用于泌尿系统、呼吸系统、胆道等感染。 Cephalosporin (头孢菌素） Decomposition of Cephalosporins in vivo Decomposed by enzyme in vivo (Inactive) (Inactive) The decoration of Cephalosporin I: Relating with the antibacterial spectrum. II:Substituted with OCH3 will stability for Bata-Lactamase III: S atom is essential for activity. IV: Relating with the antibacterial activity and bioavailibility. Semi-synthetic Cephalosprins 1.introducing lipophilic groups in 7-position( aromatic or heterocyclic rings ) R1 R2 2. introducing hydrophilic groups in α –position of 7-aimde group(-SO3H,-NH2,-COOH) will increase the antibacterial spectrum. Changing the 3-position to –CH3,-Cl will improve the bioavailibility and increase antibacterial activity. R1 R2 X 3.Introducing 2-amino-4-thiazol rings to the 7-position will increase the stabilities for Bata-Lactamase and expend the antibacterial spectrum. R1 R2 * * Antibiotics Antibiotics are microbial metabilites or synthetic analogs inspired by them that,in small doses, inhibit the growth and survival of microorganism. In clinic the antibiotics are used to be antibacterial mainly,but, in recent year, they can also be used for anti-cancer,anti-viral ,enzyme-inhibitors, and receptor-antagonist. Classification (According their structures)： 1.Beta-Lactam antibiotics (β –内酰胺类) 2.Tetracylines antibiotics (四环素类) 3.Aminoglycoside antibiotics (氨基糖甙类) 4.Macrolides antibiotics (大环内酯类) 5. Others Classification (According to their mechanism of actions Inhibit the biosynthesis of bacterial cell walls (β