Title : Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.

Pub. Date : 2002 Jun 6

PMID : 12036356






2 Functional Relationships(s)
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1 In this paper, we describe our efforts to identify an additional interaction and a replacement for the distal amidine group that binds in the S3/S4 pocket of fXa. Amidines coagulation factor X Homo sapiens
2 Introduction of a hydroxyl group para to the proximal amidine group increases the potency vs fXa by 1-2 orders of magnitude, which is the result of a hydrogen bond to Ser195 of the catalytic triad. Amidines coagulation factor X Homo sapiens