Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl- cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents

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Abstract

A novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) combinatory library was synthesized and evaluated with C8166 cells infected by the HIV-1 IIIB in vitro, using Nevirapine (NVP) and Zidovudine (AZT) as positive control. The anti-HIV screening results revealed that C-6-cyclohexylmethyl substituted pyrimidinones possessed higher selective index than its 6-arylmethyl counterparts. Compounds 1g, 1c, 1e and 1b showed potent anti-HIV activities with EC 50 values of 0.012, 0.025, 0.088 and 0.162 nM, respectively. © 2010 Elsevier Ltd. All rights reserved.

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He, Y. P., Long, J., Zhang, S. S., Li, C., Lai, C. C., Zhang, C. S., … Zheng, Y. T. (2011). Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl- cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents. Bioorganic and Medicinal Chemistry Letters, 21(2), 694–697. https://doi.org/10.1016/j.bmcl.2010.12.003

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