Abstract : 3,4-Dihydropyrimidin-2(1H)-ones (DHPMs) were selected and derivatized through a HIV-1 replication assay based on GFP reporter cells. Compounds 14, 25, 31, and 36 exhibited significant inhibition of HIV-1 replication with a good safety profile. Chiral separation of each enantiomer by fractional crystallization showed that only the S enantiomer retained anti-HIV activity. Compound (S)-40, a novel and potent DHPM analog, could serve as an advanced lead for further development and the determination of the mechanism of action.
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Junwon Kim, Changmin Park, Taedong Ok, Wonyoung So, Mina Jo, et al.. Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2012, 22 (5), pp.2119-24. ⟨10.1016/j.bmcl.2011.12.090⟩. ⟨pasteur-00683848⟩
