L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor

L-373,890, a highly selective and efficacious pyridinone acetamide thrombin inhibitor was designed using a combination of X-ray crystallography, molecular modeling and empirical structure optimization. In the first successful application of the 3-aminopyridinone acetamide template for the synthesis...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 7; no. 12; pp. 1497 - 1500
Main Authors Sanderson, Philip E.J., Dyer, Dona L., Naylor-Olsen, Adel M., Vacca, Joseph P., Gardell, Steven J., Dale Lewis, S., Lucas, Bobby J., Lyle, Elizabeth A., Lynch, Joseph J., Mulichak, Anne M.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 17.06.1997
Elsevier
Subjects
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Medical sciences
Pharmacology. Drug treatments
Sulfonamide
Serine endopeptidases
Enzyme
Nitrogen heterocycle
Peptidomimetic compound
Active site
Lactam
Enzyme inhibitor
Thrombin
Inhibitor enzyme complex
Guanidines
X ray diffraction
Modeling
Peptidases
Force field method
Piperidine derivatives
Hydrolases
Carboxamide
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Summary:L-373,890, a highly selective and efficacious pyridinone acetamide thrombin inhibitor was designed using a combination of X-ray crystallography, molecular modeling and empirical structure optimization. In the first successful application of the 3-aminopyridinone acetamide template for the synthesis of a potent, noncovalent inhibitor of either a cysteine or a serine protease, L-373,890, a highly selective and efficacious thrombin inhibitor was designed using a combination of X-ray crystallography, molecular modeling, and empirical structure optimization.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)00257-6