Synthesis and evaluation of the antiinflammatory activity of N-[2-(3,5-di-tert-butyl-4-hydroxyphenyl)-4-oxo-thiazolidin-3-yl]-nicotinamide.
A new molecule incorporating nicotinoyl moiety, thiazolidin-4-one ring and 3,5-di-tert-butyl-4-hydroxyphenyl group (a potent antioxidant moiety) was synthesized and evaluated for anti-inflammatory activity in acute as well as chronic phase models of inflammation. The compound exhibited significant anti-inflammatory activity in three experimental models of inflammation, comparable to the positive control drug, ibuprofen (CAS 15687-27-1). It is suggested that besides the hypolipidemic and anti-oxidant potential of the molecule, its anti-inflammatory action could possibly act as an additional mechanism of its hypothesized anti-atherosclerotic activity.
Kalia
Rajiv
R
Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal, India.
Rao
Chamallamudi Mallikarjuna
CM
Kutty
Nampurath Gopalan
NG
D000410:Alanine Transaminase / Q000097:blood; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D000975:Antioxidants / Q000138:chemical synthesis / Q000494:pharmacology; D001169:Arthritis, Experimental / Q000188:drug therapy / Q000473:pathology; D001219:Aspartate Aminotransferases / Q000097:blood; D050197:Atherosclerosis / Q000517:prevention & control; D002351:Carrageenan; D003300:Copper / Q000097:blood; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology; D006099:Granuloma / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology; D007052:Ibuprofen / Q000627:therapeutic use; D007202:Indicators and Reagents; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy*; D008297:Male; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D007202:Indicators and Reagents; C524550:N-(2-(3,5-di-tert-butyl-4-hydroxyphenyl)-4-oxo-thiazolidin-3-yl)-nicotinamide; D009536:Niacinamide; D003300:Copper; D002351:Carrageenan; D001219:Aspartate Aminotransferases; D000410:Alanine Transaminase; D007052:Ibuprofen