title: Design of a new prostaglandin synthetase inhibitors in a group of N-(2-carboxyphenyl)phenoxyacetamides and their antiinflammatory activity.
abstract: We propose to use in vitro tests for the design of antiinflammatory drugs. These tests are inhibition of prostaglandin synthetase and binding to albumin. The antienzymic potency of a compound is a good indicator of its local antiinflammatory activity. The difference between the antienzymic and the albumin ligand potencies of a compound roughly correlates with its systemic antiinflammatory activity. We found it rewarding to use de novo models for studying structure-activity relationship within our series of prostaglandin synthetase inhibitors. It is supposed that the general chemical character of prostaglandin synthetase inhibitors inclines to a wide application of the additive mathematical model of Free and Wilson for the design of antiinflammatory drugs.
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents; D001241:Aspirin / Q000494:pharmacology; D002417:Cattle; D016861:Cyclooxygenase Inhibitors; D006016:Glycolates / Q000494:pharmacology*; D066298:In Vitro Techniques; D007213:Indomethacin / Q000494:pharmacology; D006899:Mixed Function Oxygenases / Q000037:antagonists & inhibitors*; D010642:Phenoxyacetates / Q000494:pharmacology*; D011485:Protein Binding; D051381:Rats; D012709:Serum Albumin / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D006016:Glycolates; D010642:Phenoxyacetates; D012709:Serum Albumin; D006899:Mixed Function Oxygenases; D001241:Aspirin; D007213:Indomethacin