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Design , Synthesis and Evaluation of Some Novel 1-phenyl-3-( 5-phenyl-1 H-imidazol-1-yl ) Thiourea Derivatives as Anti-HIV Agents
| Content Provider | Semantic Scholar |
|---|---|
| Author | Singh, Rohit Ganguly, Swastika |
| Copyright Year | 2018 |
| 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. |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | https://www.ijper.org/sites/default/files/IndJPhaEdRes_52_4_655_0.pdf |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
