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

1, 1

  1. 1Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Ranchi, Jharkhand, INDIA.

CORRESPONDENCE

Rohit Singh

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

rohitsingh20485bitmesra@gmail.com

Received: 28-01-2018; Accepted: 17-05-2018.

Volume 52, Issue 4 · pp. 655-665 · 2018 · DOI: 10.5530/ijper.52.4.76

ABSTRACT

Objective: In the present study, a series of nineteen compound of 1-phenyl-3-(5-phenyl1H-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.

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    Singh, R., & Ganguly, S. (2018). Design, Synthesis and Evaluation of Some Novel 1-phenyl-3-(5-phenyl-1H-imidazol-1-yl) Thiourea Derivatives as Anti-HIV Agents.. Indian Journal of Pharmaceutical Education and Research, 52(4), 655-665. https://doi.org/10.5530/ijper.52.4.76

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    © 2018 Author(s)

    This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 License, which permits unrestricted use, distribution and reproduction in any medium, provided the original author and source are credited. CC BY 4.0