Synthesis of some new thienyl and 1,3-thiazolyl-aminoketones with anti-inflammatory activity.
Eight thienyl and 1,3-thiazolyl-aminoketones were synthesised and tested as anti-inflammatory agents. pKa and log P were theoretically calculated. The compounds were tested for antioxidant activity, as hydroxyl radical scavengers, as superoxide anion scavengers and for their ability to interact with 1,1-diphenyl-2-picryl hydrazyl stable free radical (DPPH). The effects of the synthesised compounds on inflammation were studied using the carrageenan induced mice paw oedema model. Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesised compounds.
Geronikaki
A A
AA
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Greece. geronik@pharm.auth.gr
Hadjipavlou-Litina
D J
DJ
Tzaki
M
M
D000588:Amines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015764:Bepridil / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors; D001713:Biphenyl Compounds; D002351:Carrageenan; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004121:Dimethyl Sulfoxide / Q000494:pharmacology; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D016166:Free Radical Scavengers / Q000494:pharmacology; D005609:Free Radicals / Q000737:chemistry; D017665:Hydroxyl Radical / Q000378:metabolism; D007659:Ketones / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008806:Mice, Inbred AKR; D010851:Picrates; D013329:Structure-Activity Relationship; D013481:Superoxides / Q000378:metabolism; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D014361:Trypsin Inhibitors / Q000494:pharmacology
D000588:Amines; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001713:Biphenyl Compounds; D016166:Free Radical Scavengers; D005609:Free Radicals; D007659:Ketones; D010851:Picrates; D013844:Thiazoles; D014361:Trypsin Inhibitors; D013481:Superoxides; D017665:Hydroxyl Radical; D015764:Bepridil; D002351:Carrageenan; C004931:1,1-diphenyl-2-picrylhydrazyl; D004121:Dimethyl Sulfoxide