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The discovery and synthesis of potent zwitterionic inhibitors of renin
- Source :
- Bioorganic & Medicinal Chemistry Letters. 21:2430-2436
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- The incorporation of a carboxylic acid within in a series of 3-amido-4-aryl substituted piperidines (represented by general structure 32) led to the discovery of potent, zwitterionic, renin inhibitors with improved off-target profiles (CYP3A4 time-dependent inhibition and hERG affinity) relative to analogous non-zwitterionic inhibitors of the past (i.e., 3). Strategies to address the oral absorption of these zwitterions are also discussed within.
- Subjects :
- Stereochemistry
Carboxylic acid
Clinical Biochemistry
hERG
Drug Evaluation, Preclinical
Administration, Oral
Pharmaceutical Science
Biochemistry
Chemical synthesis
Rats, Sprague-Dawley
Structure-Activity Relationship
chemistry.chemical_compound
Dogs
Piperidines
Catalytic Domain
Renin
Drug Discovery
Animals
Humans
Structure–activity relationship
Computer Simulation
Protease Inhibitors
Molecular Biology
chemistry.chemical_classification
biology
Organic Chemistry
Prodrug
Rats
Enzyme
chemistry
Enzyme inhibitor
Zwitterion
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....a5869451b5d4a9f35f5a8af8a027ba80