Design, Green Synthesis, and Anti-Inflammatory Activity of Schiff Base of 1,3,4-oxadiazole Analogues

0427576 - ÚOCHB 2015 RIV US eng J - Journal Article
Sahoo, B. M. - Dinda, S. C. - Kumar, B. V. V. R. - Panda, J. - Brahmkshatriya, Pathik
Design, Green Synthesis, and Anti-Inflammatory Activity of Schiff Base of 1,3,4-oxadiazole Analogues.
Letters in Drug Design & Discovery. Roč. 11, č. 1 (2014), s. 82-89. ISSN 1570-1808. E-ISSN 1875-628X
Institutional support: RVO:61388963
Keywords : anti-inflammatory activity * design * green synthesis * oxadiazole * schiff base * spectroscopic studies
Subject RIV: CC - Organic Chemistry
Impact factor: 0.770, year: 2014

Cyclooxygenase enzyme is a validated therapeutic target for designing drug molecules with anti-inflammatory activity. Herein, a series of various schiff base of 1,3,4-oxadiazole analogues were designed. Considering reasonable structural similarity of the target compounds with the commonly used anti-inflammatory drug indomethacin, it was decided to dock the target compounds into the active site of the molecular target of indomethacin. Prior to docking, the active sites of the proteins are identified. The docking study is performed using the UCSF DOCK 6.5 program. And also the utilization of principles involved in green chemistry is significantly reducing chemical waste and reaction times. To illustrate these advantages in the synthesis of bioactive oxadiazole derivatives, various environmentally benign protocols that involve greener alternatives were studied. The efficiency of microwave heating technology has resulted in remarkable reductions of reaction times (reduced from days and hours to minutes and seconds) with better product yield. The structures of newly synthesized compounds have been elucidated on the basis of IR, H-1 NMR, C-13 NMR, LC-MS and elemental analysis. An evaluation of the anti-inflammatory activity of the prepared compounds has indicated that some of them exhibited moderate to significant activity as compared to indomethacin.
Permanent Link: http://hdl.handle.net/11104/0233143