由青霉素制备的头孢菌素的构效关系。1. 3-苄基-和3-(3-吡啶基甲基)头孢-3-烯-4-羧酸的7β-酰氨基衍生物。
Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids.
作者信息
Brain E G, Eglington A J, Nayler J H, Osborne N F, Pearson M J, Smale T C, Southgate R, Tolliday P, Basker M J, Sutherland R
出版信息
J Med Chem. 1977 Aug;20(8):1082-5. doi: 10.1021/jm00218a018.
PMID:894679
Abstract
tert-Butyl 7beta-aminoceph-3-em-4-carboxylates carrying either benzyl or 3-pyridylmethyl substituents at position 3 have been prepared by a multistep modification of the penicillin nucleus. Acylation of either amine, followed by deprotection, gave a range of new cephalosporins. The relationship between structure and antibacterial activity is discussed. D-Phenylglycine proved to be a preferred side chain in both series.
摘要
通过青霉素母核的多步修饰制备了在3位带有苄基或3-吡啶甲基取代基的7β-氨基头孢-3-烯-4-羧酸叔丁酯。对任一胺进行酰化，然后脱保护，得到了一系列新的头孢菌素。讨论了结构与抗菌活性之间的关系。结果表明，在这两个系列中，D-苯甘氨酸都是优选的侧链。
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