Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

Back

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

Author(s): Biswa Mohan Sahoo, Subas Chandra Dinda, BVV Ravi Kumar, Jnyanaranjan Panda, Pathik S Brahmkshatriya.

Abstract:

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, 1H NMR, 13C 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.

Keywords: Anti-inflammatory activity, Design, Green synthesis, Oxadiazole, Schiff base, Spectroscopic Studies.

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 11
ISSUE: 1
Year: 2014
Page: [82 - 89]
Pages: 8
DOI: 10.2174/15701808113109990041