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受限β-链模拟物库的高效通用合成

Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.

作者信息

Ogbu C O, Qabar M N, Boatman P D, Urban J, Meara J P, Ferguson M D, Tulinsky J, Lum C, Babu S, Blaskovich M A, Nakanishi H, Ruan F, Cao B, Minarik R, Little T, Nelson S, Nguyen M, Gall A, Kahn M

机构信息

Molecumetics Ltd., Bellevue, WA 98005-2199, USA.

出版信息

Bioorg Med Chem Lett. 1998 Sep 8;8(17):2321-6. doi: 10.1016/s0960-894x(98)00420-x.

DOI:10.1016/s0960-894x(98)00420-x
PMID:9873535
Abstract

The general approach of using a bicyclic template to produce inhibitors of the protease superfamily of enzymes has been investigated. The Diels Alder cycloaddition reaction on solid support has been found to be highly efficient for the synthesis of libraries of compounds that mimic the beta-strand secondary structure of proteins. Several potent and selective inhibitors of proteases have been discovered.

摘要

研究了使用双环模板来制备蛋白酶超家族酶抑制剂的一般方法。已发现固相上的狄尔斯-阿尔德环加成反应对于合成模拟蛋白质β-链二级结构的化合物库非常有效。已发现了几种有效的蛋白酶选择性抑制剂。

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