Journal article
Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors
Bioorganic & medicinal chemistry letters, Vol.14(3), pp.667-671
2004
PMID: 14741265
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
The nonsteroidal anti-inflammatory drugs flurbiprofen and ibuprofen were modified in an attempt to alter the kinetics of inhibitor binding by COX-1. Contrary to prior predictions, a halogen substituent is not sufficient to confer slow tight-binding behavior. Conversion of the carboxylate moiety of flurbiprofen to an ester or amide abolishes slow tight-binding behavior, regardless of halogenation state.
Structure–activity relationships are reported for compounds derived from the cyclooxygenase inhibitors flurbiprofen and ibuprofen, focusing on their kinetic profiles for COX-1 inhibition.
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Details
- Title
- Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors
- Creators
- Kushol Gupta - Department of Biochemistry, Drexel University College of Medicine, Philadelphia, PA 19102, USACarl J Kaub - Department of Chemistry, Villanova University, Villanova, PA 19085, USAKristen N Carey - Department of Chemistry, Villanova University, Villanova, PA 19085, USAEduard G Casillas - Department of Chemistry, Villanova University, Villanova, PA 19085, USABarry S Selinsky - Department of Chemistry, Villanova University, Villanova, PA 19085, USAPatrick J Loll - Department of Biochemistry, Drexel University College of Medicine, Philadelphia, PA 19102, USA
- Publication Details
- Bioorganic & medicinal chemistry letters, Vol.14(3), pp.667-671
- Publisher
- Elsevier
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Biochemistry and Molecular Biology
- Identifiers
- 991014878603304721
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- Collaboration types
- Domestic collaboration
- Web of Science research areas
- Chemistry, Medicinal
- Chemistry, Organic