Potent 4-amino-5-azaindole factor VIIa inhibitors

Huiyong Hu; Aleksandr Kolesnikov; Jennifer R Riggs; Kieron E Wesson; Robin Stephens; Ellen M Leahy; William D Shrader; Paul A Sprengeler; Michael J Green; Ellen Sanford; Margaret Nguyen; Erik Gjerstad; Ronnel Cabuslay; Wendy B Young

doi:10.1016/j.bmcl.2006.06.016

Potent 4-amino-5-azaindole factor VIIa inhibitors

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4567-70. doi: 10.1016/j.bmcl.2006.06.016. Epub 2006 Jun 21.

Authors

Huiyong Hu¹, Aleksandr Kolesnikov, Jennifer R Riggs, Kieron E Wesson, Robin Stephens, Ellen M Leahy, William D Shrader, Paul A Sprengeler, Michael J Green, Ellen Sanford, Margaret Nguyen, Erik Gjerstad, Ronnel Cabuslay, Wendy B Young

Affiliation

¹ Celera Genomics, South San Francisco, CA 94080, USA. huiyong.hu@yahoo.com

PMID: 16793264
DOI: 10.1016/j.bmcl.2006.06.016

Abstract

The 4-amino-5-azaindole as an amidino-benzimidazole replacement is described. A series of potent and selective analogs were discovered and showed desirable ex vivo efficacy as measured by PT.

MeSH terms

Factor VIIa / antagonists & inhibitors*
Factor VIIa / metabolism
Indoles / chemical synthesis*
Indoles / chemistry
Indoles / pharmacology*
Molecular Structure
Pyridines / chemical synthesis*
Pyridines / chemistry
Pyridines / pharmacology*
Structure-Activity Relationship

Substances

Indoles
Pyridines
Factor VIIa