Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.
Article Details
- CitationCopy to clipboard
Gupta K, Kaub CJ, Carey KN, Casillas EG, Selinsky BS, Loll PJ
Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.
Bioorg Med Chem Lett. 2004 Feb 9;14(3):667-71.
- PubMed ID
- 14741265 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Ibuprofen Prostaglandin G/H synthase 1 Protein Humans YesInhibitorDetails Tiaprofenic acid Prostaglandin G/H synthase 1 Protein Humans YesInhibitorDetails