2008

Ring closure reactionsO 0130 Non-carboxylic Analogues of Naproxen: Design, Synthesis, and Pharmacological

Evaluation of Some 1,3,4-Oxadiazole/Thiadiazole and 1,2,4-Triazole Derivatives. — The oxadiazole, triazole, and thiadiazole nuclei are obtained either by treatment of hydrazide (II) with aromatic acids, e.g. (III), or by applying different cyclization pro-cedures to thiosemicarbazides (VI). Compounds (IV),(VII),(VIII), and (IX) show sig-nificant antiinflammatory, and, with exception of (VIIa), analgesic activity. These com-pounds reveal also ulcerogenic activity, exhibiting a significant reduction in the sever-ity index compared to the standard reference drug. Triazole (VIIb) emerges as the lead compound, displaying maximum antiinflammatory and analgesic effects along with re-duction in ulcerogenic potential and lipid peroxidation. — (AMIR*, M.; KUMAR, H.; JAVED, S. A.; Arch. Pharm. (Weinheim, Ger.) 340 (2007) 11, 577-585; Dep. Pharm. Chem., Hamdard Univ., New Delhi 110 062, India; Eng.) — H. Hoennerscheid

10- 040

2008