6533b81ffe1ef96bd1277114

RESEARCH PRODUCT

COX-1/COX-2 inhibitors based on the methanone moiety

Bernd L. FiebichGerd DannhardtJohannes Schweppenhäuser

subject

Blood PlateletsStereochemistrymedicine.drug_classDrug Evaluation PreclinicalCarboxamideIsozymeChemical synthesisStructure-Activity RelationshipOxazinesDrug DiscoverymedicineAnimalsPotencyMoietyCyclooxygenase InhibitorsPharmacologychemistry.chemical_classificationCyclooxygenase 2 InhibitorsMolecular StructurebiologyChemistryAnti-Inflammatory Agents Non-SteroidalOrganic ChemistryGeneral MedicineIn vitroIsoenzymesEnzymeCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesEnzyme inhibitorCyclooxygenase 1biology.protein

description

This paper focuses on the synthesis and the in vitro testing of dual COX-1/COX-2 inhibitors. Starting from structures of non-steroidal anti-inflammatory drugs (NSAIDs) the diaryl methanone element was chosen as a lead. Modifications were carried out on this scaffold to obtain potent inhibitors of the COX enzymes. The N-(2-aroylphenyl)sulphonamides and -amides were studied in detail, and to consolidate the data evaluated the corresponding 3- and 4-regioisomers were also investigated. The potency and the enzyme selectivity were varied by structural modifications of the lead.

yearjournalcountryeditionlanguage
2002-02-23European Journal of Medicinal Chemistry
https://doi.org/10.1016/s0223-5234(01)01330-7