Design of a new prostaglandin synthetase inhibitors in a group of N-(2-carboxyphenyl)phenoxyacetamides and their antiinflammatory activity.
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.
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
D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D006016:Glycolates; D010642:Phenoxyacetates; D012709:Serum Albumin; D006899:Mixed Function Oxygenases; D001241:Aspirin; D007213:Indomethacin