Title of article
Non-peptidic phenyl-Based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines
Author/Authors
Tianbao Lu، نويسنده , , Bruce Tomczuk، نويسنده , , Roger Bone، نويسنده , , Larry Murphy، نويسنده , , F. Raymond Salemme، نويسنده , , Richard M. Soll، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
3
From page
83
To page
85
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 title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790577
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