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Published on:June 2018
Indian Journal of Pharmaceutical Education and Research, 2018; 52(4):655-665
Original Article | doi:10.5530/ijper.52.4.76

Design, Synthesis and Evaluation of Some Novel 1-phenyl-3-(5-phenyl-1H-imidazol-1-yl) Thiourea Derivatives as Anti-HIV Agents


Authors and affiliation (s):

Rohit Singh*, Swastika Ganguly

Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Ranchi, INDIA.

Abstract:

Objective: In the present study, a series of nineteen compound of 1-phenyl-3-(5-phenyl- 1H-imidazol-1-yl) thiourea derivatives (5a-9b) were designed, synthesized, characterized by physicochemical and spectral data (IR, 1H NMR, and mass spectroscopy) and evaluated for their Anti-HIV activity with the aim to develop novel substituted imidazole derivatives with broad-spectrum chemotherapeutic properties. Methods: Compounds (5a-9b) were designed by using Glide 5.0 to carry out binding mode analysis of N-substituted imidazoles against reverse transcriptase enzyme of wild type as well as resistant strains of HIV-1 virus with PDB ID: 1RT2, synthesized by reacting various substituted anilines and substituted phenacyl bromides in four steps and evaluated their anti HIV activity as well as cytotoxicity assay through MTT colorimetric measure. Results: Compounds 6a, 6b, 6c, 6d, 7c, 9a and 9b being the most active exhibited therapeutic index that were >22.4, 31.1, 30.5, 51.5, 34.6, 30.5 and 85.6 compared to Zidovudine (AZT) having therapeutic index (TI) 514342.6. Compound 9b showed the highest docking score -12.47 in the active site of the HIV protein of 1RT2 as well better in vitro anti-HIV activity.

Key words: Molecular docking, Imidazole derivatives, Reverse transcription, Non-nucleoside reverse transcriptase inhibitors (NNRTI), Anti-HIV.

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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