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

International Journal of Molecular Sciences

Nagy M. Khalifa¹  Mohamed A. Al-Omar¹ 

[1] Pharmaceutical Chemistry Department, Drug Exploration & Development Chair, College of Pharmacy, King Saud University, Riyadh 11451, Saudia Arabia; E-Mail:

关键词: AIDS;    non-nucleoside reverse transcriptase inhibitors (NNRTIs);    2-alkylthio-6-benzylpyrimidin-4(3H)-ones (S-DABOs);    anti-HIV-1 activity;   

DOI  :  10.3390/ijms151120723

来源: mdpi

【 摘 要 】

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.

【 授权许可】

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© 2014 by the authors; licensee MDPI, Basel, Switzerland.