Phenyltriazolinones as potent factor Xa inhibitors.

Abstract:

:We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate.

journal_name

Bioorg Med Chem Lett

authors

Quan ML,Pinto DJ,Rossi KA,Sheriff S,Alexander RS,Amparo E,Kish K,Knabb RM,Luettgen JM,Morin P,Smallwood A,Woerner FJ,Wexler RR

doi

10.1016/j.bmcl.2010.01.011

subject

Has Abstract

pub_date

2010-02-15 00:00:00

pages

1373-7

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00013-2

journal_volume

20

pub_type

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