AI Article Synopsis
- A new library of compounds called S-DACOs was created and tested against HIV-1 infected C8166 cells, using Nevirapine and Zidovudine as controls.
- * The screening found that pyrimidinones with a cyclohexylmethyl group at C-6 had better efficacy than those with an arylmethyl group.
- * Four specific compounds (1g, 1c, 1e, and 1b) demonstrated strong anti-HIV effects, with EC(50) values ranging from 0.012 to 0.162 nM.
Article 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 0.162nM, respectively.
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| http://dx.doi.org/10.1016/j.bmcl.2010.12.003 | DOI Listing |
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