Burton G, Clear N J, Eglington A J, Guest A W, Hunt E, Naylor A, Pearson M J, Takle A K
SmithKline Beecham Pharmaceuticals, Brockham Park, Betchworth, Surrey, U.K.
J Antibiot (Tokyo). 1996 Dec;49(12):1258-65. doi: 10.7164/antibiotics.49.1258.
A new series of carbapenems, having a saturated or partially unsaturated heterocycle at C-2, has been synthesised. The in vitro antibacterial activity of these compounds and their stability to human dehydropeptidase-1 (DHP-1) are described. The stereochemistry of the C-2 side-chain and the presence of a double bond in the heterocycle were shown to have significant effects on the stabilities of the compounds to DHP-1.
已经合成了一系列新的碳青霉烯类化合物,其在C-2位具有饱和或部分不饱和的杂环。描述了这些化合物的体外抗菌活性及其对人脱氢肽酶-1(DHP-1)的稳定性。结果表明,C-2侧链的立体化学和杂环中双键的存在对化合物对DHP-1的稳定性有显著影响。