Synthesis and Biological Evaluation of Novel Hydroxylphenethyl-SDACOs as High Active Anti-HIV Agents

Author(s): Dao-Chun Wu, Dao-Ming Zhuang, Xiao-Feng Liu, Li-He Lu, Hua Wang, Cong Li, Christopher Cong Lai, Jing-Yun Li, Yan-Ping He.

Journal Name: Letters in Drug Design & Discovery

Volume 10 , Issue 3 , 2013

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A novel 5-alky-6-(cyclohexylmethyl)-2-((2-hydroxy-2-phenylethyl)thio)-pyrimidin-4(3H)-one derivatives were synthesized and their ability to inhibit HIV evaluated . The screening results revealed that compounds 2a-g had a favorable property in inhibiting HIV. The compounds 2b, in particular, showed a special potent anti-HIV activities with EC50 values of 0.003μM and CC50 values of 200 μM. Preliminary structure-activity relationship (SAR) and molecular modeling analyses of these newly synthesized hydroxylphenethyl-S-DACOs are also discussed.

Keywords: Anti HIV-1 activity; Water-solubility; Molecular Docking; NNRTIs; Pyrimidone; S-DACOs.

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Article Details

Year: 2013
Page: [271 - 276]
Pages: 6
DOI: 10.2174/1570180811310030011
Price: $58

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