New 1,3,4-oxadiazole/oxime hybrids: Design, synthesis, anti-inflammatory, COX inhibitory activities and ulcerogenic liability

作者：Abd Ellah Heba S; Abdel Aziz Mohamed; Shoman Mai E^*; Beshr Eman A M; Kaoud TamerS; Ahmed Al Shaimaa F F

来源：Bioorganic Chemistry, 2017, 74: 15-29.

DOI：10.1016/j.bioorg.2017.06.003

• 1,3,4-Oxadiazole
• Nitric oxide
• Anti-inflammatory
• Anti-oxidant activity

A series of new 1,3,4-oxadiazole/oxime hybrids were synthesized and designed as potent COX inhibitors. The prepared compounds were evaluated for their anti-inflammatory, antioxidant and ulcerogenic activities. The results indicated that the prepared compounds exhibited remarkable anti-inflammatory activity with (69.60-109.60% of indomethacin activity) after 4 h. In vitro COX inhibitory assay showed that compounds 6d and 7h are potent COX inhibitors with IC50 of (1.10-0.94) and (2.30-5.00) mM on both COX-1 and COX-2 respectively. Compound 7h was found to inhibit both COXs non-competitively with K-i values of 73 mM and 89 mM. Most of the tested compounds showed ulcer-free stomachs compared to indomethacin.

• 出版日期2017-10