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Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.

Abstract：

:We expand the structural requirements and structure-activity relationship of a novel class of non-peptidic aryl-based thrombin inhibitors through exploration of the S1 specificity pocket of thrombin using flexible and constrained amidines. The most active compound of this class is 11 with Ki = 69 nM, which is ca. 15-fold less potent than constrained guanidine 5.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lu T,Tomczuk B,Bone R,Murphy L,Salemme FR,Soll RM

doi

10.1016/s0960-894x(99)00616-2

subject

Has Abstract

pub_date

2000-01-03 00:00:00

pages

83-5

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(99)00616-2

journal_volume

10

pub_type

杂志文章

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