The discovery and development of 5-azaindole factor VIIa inhibitors will be described.
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Structure-based design and optimization of potent renin inhibitors on 5- or 7-azaindole-scaffolds.
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Sanofi-Aventis Deutschland GmbH, Chemical and Analytical Sciences, Building G878, D-65926 Frankfurt, Germany.
The selective inhibition of the aspartyl protease renin is of high interest to control hypertension and associated cardiovascular risk factors. Following on preceding contributions, we report herein on the optimization of two series of azaindoles to arrive at potent and non-chiral renin inhibitors. The previously discovered azaindole scaffold was further explored by structure-based drug design in combination with parallel synthesis.
View Article and Find Full Text PDFPotent 4-amino-5-azaindole factor VIIa inhibitors.
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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.
View Article and Find Full Text PDFNovel 5-azaindole factor VIIa inhibitors.
Bioorg Med Chem Lett
June 2006
Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA.
The discovery and development of 5-azaindole factor VIIa inhibitors will be described.
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