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

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

Volume: 10 Issue: 3

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Wu Dao-Chun, Zhuang Dao-Ming, Liu Xiao-Feng, Lu Li-He, Wang Hua, Li Cong, Cong Lai Christopher, Li Jing-Yun and He Yan-Ping, Synthesis and Biological Evaluation of Novel Hydroxylphenethyl-SDACOs as High Active Anti-HIV Agents, Letters in Drug Design & Discovery 2013; 10 (3) . https://dx.doi.org/10.2174/1570180811310030011