Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site

E Vieira; A Binggeli; V Breu; D Bur; W Fischli; R Güller; G Hirth; H P Märki; M Müller; C Oefner; M Scalone; H Stadler; M Wilhelm; W Wostl

doi:10.1016/s0960-894x(99)00195-x

Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site

Bioorg Med Chem Lett. 1999 May 17;9(10):1397-402. doi: 10.1016/s0960-894x(99)00195-x.

Authors

E Vieira¹, A Binggeli, V Breu, D Bur, W Fischli, R Güller, G Hirth, H P Märki, M Müller, C Oefner, M Scalone, H Stadler, M Wilhelm, W Wostl

Affiliation

¹ Pharma Research Department, F. Hoffmann-La Roche Ltd, Basel, Switzerland.

PMID: 10360744
DOI: 10.1016/s0960-894x(99)00195-x

Abstract

The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified.

MeSH terms

Binding Sites
Humans
Models, Molecular
Molecular Structure
Piperidines / chemistry
Piperidines / metabolism
Piperidines / pharmacology*
Recombinant Proteins / antagonists & inhibitors
Recombinant Proteins / metabolism
Renin / antagonists & inhibitors*
Renin / metabolism

Substances

Piperidines
Recombinant Proteins
Renin