Utilizing X-ray crystal structure analysis,(3S, 5R)-5-[4-(2-chlorophenyl)-2, 2-dimethyl-5-
oxopiperazin-1-yl] piperidine-3-carboxamides were designed and identified as renin …

We report synthesis and optimization of a series of (3S, 5R)-5-(2, 2-dimethyl-5-oxo-4-
phenylpiperazin-1-yl) piperidine-3-carboxamides as renin inhibitors. Chemical modification …

We previously identified 2-tert-butyl-4-[(3-methoxypropyl) amino]-N-(2-methylpropyl)-N-[(3S,
5R)-5-(morpholin-4-ylcarbonyl) piperidin-3-yl] pyrimidine-5-carboxamide 3 as a potent renin …

The discovery and SAR of a series of potent renin inhibitors possessing a novel 3, 4-
diarylpiperidine scaffold are described herein. The resulting compound 38 exhibit low …

Introduction of the 2, 2-dimethyl-4-phenylpiperazin-5-one scaffold into the P3–P1 portion of
the (2S, 4S, 5S)-5-amino-6-dialkylamino-4-hydroxy-2-isopropylhexanamide backbone …

The optimization of the 4-position of recently described new 3, 4-disubstituted piperidine-
based renin inhibitors is reported herein. The synthesis and characterization of compounds …

The action of the aspartyl protease renin is the rate-limiting initial step of the renin-
angiotensin-aldosterone system. Therefore, renin is a particularly promising target for blood …

Starting from known piperidine renin inhibitors, a new series of 3, 9-diazabicyclo [3.3. 1]
nonene derivatives was rationally designed and prepared. Optimization of the positions 3, 6 …

The discovery of a new series of piperidine-based renin inhibitors is described herein. SAR
optimization upon the P3 renin sub-pocket is described, leading to the discovery of 9 and 41 …

The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl
scaffold are described herein. Molecular modeling revealed that the cyclopropylamide …