Synthesis of combinatorial libraries of 3,4,5-trisubstituted 2(5H)-furanones. Part Two: Construction of a library of 4-amino-5-alkoxy-2(5H)-furanones.

Drug design and discovery Pub Date : 1999-11-01
E Lattmann, D C Billington, C A Langley
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引用次数: 0

Abstract

A three dimensional combinatorial library of 3-halogen-4-amino-5-alkoxy-2(5H)-furanones has been prepared by applying solution phase combinatorial chemistry techniques. The substituents in the 3-4-5-positions of a butenolide scaffold were varied independently to generate with 3 butenolides, 4 alcohols and 24 amines a library of 288 compounds using a 2 stage synthetic protocol. Typical representives of the library were purified and fully characterized. Biological evaluation resulted in the discovery of a lead structure for a new class of antibiotic agents. The 4-benzylamino-2(5H)-furanone, Dr, of this library has shown a promising antibiotic activity against the multiresistant Staphillococcus aureus (MRSA 96-7778).

3,4,5-三取代2(5H)-呋喃酮组合文库的合成。第二部分:4-氨基-5-烷氧基-2(5H)-呋喃酮文库的构建。
采用液相组合化学技术制备了3-卤素-4-氨基-5-烷氧基-2(5H)-呋喃酮的三维组合文库。丁烯内酯支架的3-4-5位取代基独立变化,以3个丁烯内酯、4个醇类和24个胺类化合物为原料,采用2段合成方案合成288个化合物。对文库的典型代表进行了纯化并进行了充分的表征。生物评价的结果是发现了一类新型抗生素的先导结构。该文库的4-苄基氨基-2(5H)-呋喃酮博士已显示出对多重耐药金黄色葡萄球菌(MRSA 96-7778)的有希望的抗生素活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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