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Vol. 31 No. 9 (2019): Vol 31 Issue 9

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Docking, Synthesis and Biological Evaluation of Novel Diketoquinoline Analogues as HIV-1 Integrase Inhibitor

https://doi.org/10.14233/ajchem.2019.22045
Kishore D. Deo
Department of Pharmacy, Pacific Academy of Higher Education and Research University, Udaipur-313003, India
I.J. Singhvi
Department of Pharmacy, Pacific Academy of Higher Education and Research University, Udaipur-313003, India
S.R. Patil
M.G.S.M. Arts, Science and Commerce College, Chopda-425107, India
Avinash V. Patil
Smt. S.S. Patil College of Pharmacy, Chopda-425107, India

Corresponding Author(s) : Avinash V. Patil

avinashay_princ@rediffmail.com

Asian Journal of Chemistry, Vol. 31 No. 9 (2019): Vol 31 Issue 9

Abstract

A series of novel diketoquinoline acid derivatives as potential anti-HIV-1 Integrase inhibitors were docked, synthesized and characterized by IR, NMR , CHN and MS spectral analysis. Many compounds were identified and docked in integrase pocket. The target diketoquinolines were prepared from substituted oxoquinoline-3-carboxylate. In vitro biological evaluation revealed that some of the titled compounds exhibited moderate to good anti-HIV-1 Integrase inhibitory activity in comparison with the reference drugs i.e. raltegravir and nevirapine. The cytotoxicity of most of testing compounds on C8166 were very low, the CC50 value of them were higher than 200 μM, except the few compounds. Compounds 1-5 showed weak anti-HIV-1 activity, its therapeutic index was 457, 531, 583, 869 and 909 respectively. As a positive control drug, Nevirapine has the best anti-HIV-1 activity (EC50 = 0.015-0.016 μM) in vitro and the CC50 of was higher than 200 μM, its therapeutic index was higher 12418.50. In integrase assay compound 6 and 7 showed EC50 value 0.08 μM as compared with standard drug raltegravir.

Keywords

Elvitegravir Diketoquinoline Docking HIV-1 integrase Raltegravir Nevirapine Syncytium
Deo, K. D., Singhvi, I., Patil, S., & Patil, A. V. (2019). Docking, Synthesis and Biological Evaluation of Novel Diketoquinoline Analogues as HIV-1 Integrase Inhibitor. Asian Journal of Chemistry, 31(9), 2000–2008. https://doi.org/10.14233/ajchem.2019.22045
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