Non-carboxylic analogues of arylpropionic acids: synthesis, anti-inflammatory activity and ulcerogenic potential.
Two series of 1,2,4-triazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles derived from three selected arylpropionic acids namely, ibuprofen, flurbiprofen and naproxen, were synthesized and evaluated for anti-inflammatory activity and ulcerogenic potential. All the tested compounds exhibited anti-inflammatory activity comparable to that of hydrocortisone. Compared to ibuprofen, however, all the tested compounds displayed more potent anti-inflammatory activity. Compounds tested for ulcerogenicity showed no or minimal ulcerogenic effect compared to indomethacin.
Metwally
Kamel A
KA
Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. kametwally@hotmail.com <kametwally@hotmail.com>
Yaseen
Shada H
SH
Lashine
El-Sayed M
el-SM
El-Fayomi
Hassan M
HM
El-Sadek
Mohamed E
ME
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D005480:Flurbiprofen / Q000737:chemistry; D007052:Ibuprofen / Q000737:chemistry; D008297:Male; D009288:Naproxen / Q000737:chemistry; D011422:Propionates / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011422:Propionates; D013830:Thiadiazoles; D013844:Thiazoles; D009288:Naproxen; D005480:Flurbiprofen; D007052:Ibuprofen