Research Article | Volume: 8, Issue: 11, November, 2018

Design, synthesis, and biological evaluation of 2-(4-(methylsulfonyl) phenyl) indole derivatives with promising COX-2 inhibitory activity

Ahmed M. M. Shaker Eman K. A. Abdelall Khaled R. A. Abdellatif  Hamdy M. Abdel-Rahman   

Open Access   

Published:  Nov 30, 2018

DOI: 10.7324/JAPS.2018.81101

A series of 2-(4-(methylsulfonyl)phenyl)-1-substituted-indole derivatives 4a–f was designed and synthesized as indomethacin analogs; All synthesized compounds were assessed for their in vitro COX-2 inhibition effect as well as in vivo anti-inflammatory activity using indomethacin as a reference drug. All synthesized compounds showed good anti-inflammatory activity and more selectivity for COX-2 inhibition. A molecular modeling study was carried out and the results were compatible with that derived from in vitro COX-2 inhibition assays.

Keyword:     Indole indomethacin anti-inflammatory activity selective COX-2 molecular modeling.


Shaker AMM, Abdelall EKA, Abdellatif KRA, AbdelRahman HM. Design, synthesis and biological evaluation of 2-(4-(methylsulfonyl)phenyl) indole derivatives with promising COX-2 inhibitory activity. J App Pharm Sci, 2018; 8(11): 001–008.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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