Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors

Substituted pyrazoles, 1,2,4-triazoles, and tetrazoles are good surrogates for cis-amide bonds in a series of boronate ester thrombin inhibitors. Substituted pyrazoles, 1,2,4-triazoles, and tetrazoles are good surrogates for cis-amide bonds in a series of boronate ester thrombin inhibitors.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-04, Vol.8 (7), p.775-780
Main Authors: Duncia, John V., Santella, Joseph B., Anne Higley, C., VanAtten, Mary K., Weber, Patricia C., Alexander, Richard S., Kettner, Charles A., Pruitt, James R., Liauw, Anne Y., Quan, Mimi L., Knabb, Robert M., Wexler, Ruth R.
Format: Article
Language:English
Subjects:
Amides - chemistry
Amides - pharmacology
Binding Sites
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Boronic Acids - chemistry
Boronic Acids - pharmacology
Crystallography, X-Ray
Indicators and Reagents
Medical sciences
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacology
Stereoisomerism
Structure-Activity Relationship
Tetrazoles - chemical synthesis
Tetrazoles - chemistry
Tetrazoles - pharmacology
Thrombin - antagonists & inhibitors
Thrombin - chemistry
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - pharmacology
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Summary:Substituted pyrazoles, 1,2,4-triazoles, and tetrazoles are good surrogates for cis-amide bonds in a series of boronate ester thrombin inhibitors. Substituted pyrazoles, 1,2,4-triazoles, and tetrazoles are good surrogates for cis-amide bonds in a series of boronate ester thrombin inhibitors.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00104-8