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Design, Green Synthesis, and Anti-Inflammatory Activity of Schiff Base of 1,3,4-oxadiazole Analogues
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SYSNO ASEP 0427576 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Design, Green Synthesis, and Anti-Inflammatory Activity of Schiff Base of 1,3,4-oxadiazole Analogues Author(s) Sahoo, B. M. (IN)
Dinda, S. C. (IN)
Kumar, B. V. V. R. (IN)
Panda, J. (IN)
Brahmkshatriya, Pathik (UOCHB-X)Number of authors 5 Source Title Letters in Drug Design & Discovery - ISSN 1570-1808
Roč. 11, č. 1 (2014), s. 82-89Number of pages 8 s. Language eng - English Country US - United States Keywords anti-inflammatory activity ; design ; green synthesis ; oxadiazole ; schiff base ; spectroscopic studies Subject RIV CC - Organic Chemistry Institutional support UOCHB-X - RVO:61388963 UT WOS 000327727900012 EID SCOPUS 84889604863 DOI 10.2174/15701808113109990041 Annotation 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Year of Publishing 2015
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