Multicomponent Reaction for Synthesis, Molecular Docking and Anti-inflammatory Evaluation of Novel Indole-Thiazole Hybrid Derivatives

Author:

Alkorbi Faeza1,Alshareef Shareefa Ahmed2,Abdelaziz Mahmoud A.2,Omer Noha2,Jame Rasha2,Alatawi Ibrahim Saleem2,Ali Ali M.3,Omran Omran A.3,Bakr Rania B.4

Affiliation:

1. Najran University

2. University of Tabuk

3. Sohag University

4. Beni-Suef University

Abstract

Abstract

In this article, novel thiazol-indolin-2-one derivatives 4a-f have been synthesized via treatment of thiosemicarbazide (1) with some isatin derivative 2a-f and N-(4-(2-bromoacetyl)phenyl)-4-tolyl-sulfonamide (3) under reflux in ethanol in the presence of triethyl amine (TEA). The structures of new products were elucidated by elemental and spectral analyses. Moreover, all compounds were investigated for their in vivo anti-inflammatory activity using celecoxib as a reference drug. The target comound 4b was the most active anti-inflammatory candidate and exhibited higher edema inhibition (EI = 38.50 %) than that recorded by celecoxib (EI = 34.58%) after 3h. Furthermore, the most active compounds 4band 4f were subjected to molecular docking study inside COX-2 enzyme to show their binding interactions. Both compounds 4b and 2f showed good fitting into COX-2 binding site with docking energy scores -11.45 kcal/mol and -10.48kcal/mol,respectively which indicated that compound 4b revealed the most promising and effective anti-inflammatory potential.

Publisher

Springer Science and Business Media LLC

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