Abstract
The design and optimization of a novel series of renin inhibitor is described herein. Strategically, by committing the necessary resources to the development of synthetic sequences and scaffolds that were most amenable for late stage structural diversification, even as the focus of the SAR campaign moved from one end of the molecule to another, highly potent renin inhibitors could be rapidly identified and profiled.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Alcohols / chemical synthesis*
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Alcohols / chemistry
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Alcohols / therapeutic use
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Animals
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Antihypertensive Agents / chemical synthesis*
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Antihypertensive Agents / chemistry
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Antihypertensive Agents / therapeutic use*
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Drug Design*
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Hypertension / drug therapy*
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Molecular Structure
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / therapeutic use
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Rats
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Renin / antagonists & inhibitors*
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Renin / chemistry
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Structure-Activity Relationship
Substances
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Alcohols
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Antihypertensive Agents
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Piperidines
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Renin