2-（磺酰胺基）甲基碳青霉烯类的合成与活性：新型抗耐甲氧西林金黄色葡萄球菌1,8-萘磺内酰胺药效团的发现

Synthesis and activity of 2-(sulfonamido)methyl-carbapenems: discovery of a novel, anti-MRSA 1,8-naphthosultam pharmacophore.

作者信息

Wilkening R R, Ratcliffe R W, Wildonger K J, Cama L D, Dykstra K D, DiNinno F P, Blizzard T A, Hammond M L, Heck J V, Dorso K L, St Rose E, Kohler J, Hammond G G

机构信息

Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., Rahway, New Jersey 07065-0900, USA.

出版信息

Bioorg Med Chem Lett. 1999 Mar 8;9(5):673-8. doi: 10.1016/s0960-894x(99)00070-0.

DOI:10.1016/s0960-894x(99)00070-0

PMID:10201827

Abstract

A series of 1beta-methyl carbapenems substituted at the 2-position with lipophilic, acyclic and cyclic (sulfonamido)methyl groups was prepared and evaluated for activity against resistant gram-positive bacteria. From these studies, the 1,8-naphthosultamyl group emerged as a novel, PBP2a-binding, anti-MRSA pharmacophore worthy of further exploration.

摘要

制备了一系列在2位被亲脂性、无环和环状（磺酰胺基）甲基取代的1β-甲基碳青霉烯类化合物，并评估了它们对耐药革兰氏阳性菌的活性。通过这些研究，1,8-萘磺酰胺基作为一种新型的、结合PBP2a的抗耐甲氧西林金黄色葡萄球菌药效基团而出现，值得进一步探索。