Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.

Article Details

Citation

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
DrugTargetKindOrganismPharmacological ActionActions
IbuprofenProstaglandin G/H synthase 1ProteinHumans
Yes
Inhibitor
Details
Tiaprofenic acidProstaglandin G/H synthase 1ProteinHumans
Yes
Inhibitor
Details