5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa

Structural features of a 5-amidinoindole inhibitor of factor Xa, which displayed modest inhibition of factor IXa were varied to increase potency and improve selectivity for factor IXa.

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 14; no. 21; pp. 5269 - 5273
Main Authors Batt, Douglas G, Qiao, Jennifer X, Modi, Dilip P, Houghton, Gregory C, Pierson, Deborah A, Rossi, Karen A, Luettgen, Joseph M, Knabb, Robert M, Jadhav, P K, Wexler, Ruth R
Format Journal Article
LanguageEnglish
Published England 01.11.2004
Subjects
Factor IXa - antagonists & inhibitors
Factor IXa - chemistry
Factor Xa - chemistry
Factor Xa Inhibitors
Indoles - chemical synthesis
Indoles - chemistry
Models, Molecular
Stereoisomerism
Structure-Activity Relationship
Substrate Specificity
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Summary:Structural features of a 5-amidinoindole inhibitor of factor Xa, which displayed modest inhibition of factor IXa were varied to increase potency and improve selectivity for factor IXa.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.08.037