Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives
In the present study, a series of fourteen 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives were designed, synthesized and characterized by appropriate spectral analysis. Further, titled compounds were in-vitro screened against wild HIV-1 RT enzyme using ELISA based color...
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| Format: | Article |
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Academic Press Inc.
2017
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| _version_ | 1796862342387990528 |
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| author | Chander, S. Tang, C. R. Al Maqtari, H. M. Jamalis, J. Penta, A. Hadda, T. B. Sirat, H. M. Zheng, Y. T. Sankaranarayanan, M. |
| author_facet | Chander, S. Tang, C. R. Al Maqtari, H. M. Jamalis, J. Penta, A. Hadda, T. B. Sirat, H. M. Zheng, Y. T. Sankaranarayanan, M. |
| author_sort | Chander, S. |
| collection | ePrints |
| description | In the present study, a series of fourteen 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives were designed, synthesized and characterized by appropriate spectral analysis. Further, titled compounds were in-vitro screened against wild HIV-1 RT enzyme using ELISA based colorimetric assay, in which four compounds significantly inhibited the RT activity with IC50 ≤ 25 µM. Moreover, two significantly active compounds of the series, A10 and A11 exhibited IC50 values 8.62 and 6.87 µM respectively, during the in-vitro assay. Structure Activity Relationship (SAR) studies were performed for the synthesized compounds in order to estimate the effect of substitution pattern on the RT inhibitory potency. The cytotoxicity of the synthesized compounds was evaluated against T lymphocytes. Further, putative binding modes of the significantly active (A11) and the least active (A4) compounds with wild HIV-1 RT were also investigated using docking studies. |
| first_indexed | 2024-03-05T20:10:11Z |
| format | Article |
| id | utm.eprints-75438 |
| institution | Universiti Teknologi Malaysia - ePrints |
| last_indexed | 2024-03-05T20:10:11Z |
| publishDate | 2017 |
| publisher | Academic Press Inc. |
| record_format | dspace |
| spelling | utm.eprints-754382019-02-13T07:00:59Z http://eprints.utm.my/75438/ Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives Chander, S. Tang, C. R. Al Maqtari, H. M. Jamalis, J. Penta, A. Hadda, T. B. Sirat, H. M. Zheng, Y. T. Sankaranarayanan, M. QD Chemistry In the present study, a series of fourteen 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives were designed, synthesized and characterized by appropriate spectral analysis. Further, titled compounds were in-vitro screened against wild HIV-1 RT enzyme using ELISA based colorimetric assay, in which four compounds significantly inhibited the RT activity with IC50 ≤ 25 µM. Moreover, two significantly active compounds of the series, A10 and A11 exhibited IC50 values 8.62 and 6.87 µM respectively, during the in-vitro assay. Structure Activity Relationship (SAR) studies were performed for the synthesized compounds in order to estimate the effect of substitution pattern on the RT inhibitory potency. The cytotoxicity of the synthesized compounds was evaluated against T lymphocytes. Further, putative binding modes of the significantly active (A11) and the least active (A4) compounds with wild HIV-1 RT were also investigated using docking studies. Academic Press Inc. 2017 Article PeerReviewed Chander, S. and Tang, C. R. and Al Maqtari, H. M. and Jamalis, J. and Penta, A. and Hadda, T. B. and Sirat, H. M. and Zheng, Y. T. and Sankaranarayanan, M. (2017) Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives. Bioorganic Chemistry, 72 . pp. 74-79. ISSN 0045-2068 https://dx.doi.org/10.1016/j.bioorg.2017.03.013 DOI:10.1016/j.bioorg.2017.03.013 |
| spellingShingle | QD Chemistry Chander, S. Tang, C. R. Al Maqtari, H. M. Jamalis, J. Penta, A. Hadda, T. B. Sirat, H. M. Zheng, Y. T. Sankaranarayanan, M. Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives |
| title | Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives |
| title_full | Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives |
| title_fullStr | Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives |
| title_full_unstemmed | Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives |
| title_short | Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives |
| title_sort | synthesis and study of anti hiv 1 rt activity of 5 benzoyl 4 methyl 1 3 4 5 tetrahydro 2h 1 5 benzodiazepin 2 one derivatives |
| topic | QD Chemistry |
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