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开发一种用于N-取代泛酰胺平行合成和纯化的方法,N-取代泛酰胺是已知的辅酶A生物合成和利用的抑制剂。

Development of a method for the parallel synthesis and purification of N-substituted pantothenamides, known inhibitors of coenzyme A biosynthesis and utilization.

作者信息

van Wyk Marianne, Strauss Erick

机构信息

Department of Biochemistry, Stellenbosch University, Matieland 7602, South Africa.

出版信息

Org Biomol Chem. 2008 Dec 7;6(23):4348-55. doi: 10.1039/b811086g. Epub 2008 Oct 17.

Abstract

N-Substituted pantothenamides are a class of pantothenic acid analogues which have been shown to act as inhibitors of coenzyme A biosynthesis and utilization, especially by blocking fatty acid metabolism through formation of inactive acyl carrier proteins. To fully explore the chemical diversity and inhibitory potential of these analogues we have developed a simple method for the parallel synthesis and purification of any number of pantothenamides from a single precursor, and subsequently evaluated a small library of these compounds as inhibitors of bacterial growth to demonstrate the potential and utility of the method.

摘要

N-取代泛酰胺是一类泛酸类似物,已被证明可作为辅酶A生物合成和利用的抑制剂,特别是通过形成无活性的酰基载体蛋白来阻断脂肪酸代谢。为了全面探索这些类似物的化学多样性和抑制潜力,我们开发了一种简单的方法,可从单一前体并行合成和纯化任意数量的泛酰胺,随后评估了这些化合物的一个小型文库作为细菌生长抑制剂,以证明该方法的潜力和实用性。

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