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琥珀酰氧肟酸及其羧酸类似物对基质金属蛋白酶MMP - 3和MMP - 2抑制作用的选择性取决于P3'基团的手性。

Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality.

作者信息

Fray M J, Burslem M F, Dickinson R P

机构信息

Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent, UK.

出版信息

Bioorg Med Chem Lett. 2001 Feb 26;11(4):567-70. doi: 10.1016/s0960-894x(00)00719-8.

DOI:10.1016/s0960-894x(00)00719-8
PMID:11229773
Abstract

Structure-activity relationships are described for a series of succinyl hydroxamic acids 1a-o and their carboxylic acid analogues 2a-o as inhibitors of matrix metalloproteases MMP-3 and MMP-2. For this series (P1' = (CH2)3Ph, P2' = t-Bu) selectivity for the inhibition of MMP-2 was found to be strongly dependent on P3'.

摘要

描述了一系列琥珀酰氧肟酸1a - o及其羧酸类似物2a - o作为基质金属蛋白酶MMP - 3和MMP - 2抑制剂的构效关系。对于该系列（P1' = (CH2)3Ph，P2' = t - Bu），发现对MMP - 2抑制的选择性强烈依赖于P3'。

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