Synthesis of some new 2-(2-fluoro-4-biphenylyl)propionic acid derivatives as potential anti-inflammatory agents.
The synthesis of a group of 1,3,4-oxadiazoles, 1,2,4-triazoles, 1,3,4-thiadiazoles and 1,2,4-triazine derived from 2-(2-fluoro-4-biphenylyl) propionic acid is described. The structures of new compounds are supported by IR, 1H NMR and MS data. These compounds were tested in vivo for their anti-inflammatory activity. The compounds which showed activity comparable to the standard drug flurbiprofen, were screened for their analgesic, ulcerogenic and lipid peroxidation activities. Five out of seventeen new compounds, showed very good anti-inflammatory activity in the carrageenan induced rat paw edema test with negligible ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde production (MDA), which is one of the byproducts of lipid peroxidation. The study showed that the compounds inhibit the induction of gastric mucosal lesions and it can be suggested from our results that their protective effects may be related to an inhibition of lipid peroxidation in the gastric mucosa.
Amir
M
M
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi, India. mamir_s2003@yahoo.co.in
Kumar
S
S
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D005480:Flurbiprofen / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D005528:Foot / Q000473:pathology; D007202:Indicators and Reagents; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D010147:Pain Measurement / Q000187:drug effects; D011422:Propionates / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001713:Biphenyl Compounds; D007202:Indicators and Reagents; D011422:Propionates; D005480:Flurbiprofen; D002351:Carrageenan