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Int. J. Mol. Sci. 2014, 15(11), 20723-20735; doi:10.3390/ijms151120723

Synthesis and Biological Evaluation of 2-Thioxopyrimidin-4(1H)-one Derivatives as Potential Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

1
Pharmaceutical Chemistry Department, Drug Exploration & Development Chair, College of Pharmacy, King Saud University, Riyadh 11451, Saudia Arabia
2
Therapeutical Chemistry Department, Pharmaceutical and Drug Industries Division, National Research Centre, Dokki 12622, Cairo, Egypt
*
Author to whom correspondence should be addressed.
Received: 5 September 2014 / Revised: 18 October 2014 / Accepted: 3 November 2014 / Published: 12 November 2014
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
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Abstract

A series of new 5-allyl-6-benzylpyrimidin-4(3H)-ones bearing different substituents at the C-2 position of the pyrimidine core have been synthesized and evaluated for their in vitro activities against human immunodeficiency virus type 1 (HIV-1) in the human T-lymphotropic type (MT-4 cell cultures). The majority of the title compounds showed moderate to good activities against HIV-1. Amongst them, 5-allyl-6-benzyl-2-(3-hydroxypropylthio)pyrimidin-4(3H)-one analogue 11c exhibited the most potent anti-HIV-1 activity (IC50 0.32 µM). The biological testing results clearly indicated that the substitution at C-2 position of the pyrimidine ring could increase the anti-HIV-1 reverse transcriptase (RT) activity. View Full-Text
Keywords: AIDS; non-nucleoside reverse transcriptase inhibitors (NNRTIs); 2-alkylthio-6-benzylpyrimidin-4(3H)-ones (S-DABOs); anti-HIV-1 activity AIDS; non-nucleoside reverse transcriptase inhibitors (NNRTIs); 2-alkylthio-6-benzylpyrimidin-4(3H)-ones (S-DABOs); anti-HIV-1 activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Khalifa, N.M.; Al-Omar, M.A. Synthesis and Biological Evaluation of 2-Thioxopyrimidin-4(1H)-one Derivatives as Potential Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors. Int. J. Mol. Sci. 2014, 15, 20723-20735.

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