论文部分内容阅读
40年前,β-内酰胺类抗生素在治疗感染症中的位置已被确定,现在它们所占费用是抗生素费用160亿美元的一半以上。目前使用的约60个β-内酰胺抗生素是由6-氨基青霉烷酸(6-APA)或7-氨基头孢烷酸(7-ACA),经氨基酸化制备得到。由于6-APA和7-ACA的可用性,酰化工艺的简单性,以及抗菌性能可变性导致半合成青霉素和头孢菌素的广泛使用。 6-取代青霉素 Beecham对青霉素的兴趣是众所周知的,其中广泛使用的羟氨苄青霉素和替卡西林是该公司的实验室在1957年6-APA分离后首次制成的。1970年该公司决定了从x替
40 years ago, the location of beta-lactam antibiotics in the treatment of infectious diseases has been identified, and now they account for more than half of the cost of antibiotics for more than $ 16 billion. Approximately 60 β-lactam antibiotics currently used are prepared by amino acidization of 6-aminopenicillanic acid (6-APA) or 7-aminocephalosporanic acid (7-ACA). Due to the availability of 6-APA and 7-ACA, the simplicity of the acylation process and the variability of antibacterial properties lead to the widespread use of semi-synthetic penicillins and cephalosporins. 6-Substituted penicillin Beecham’s interest in penicillin is well known, with amoxicillin and ticarcillin widely used by the company’s laboratories being first made after the 6-APA separation in 1957. The company decided in 1970 to replace x