Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593834 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
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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Authors
Junwon Kim, Changmin Park, Taedong Ok, Wonyoung So, Mina Jo, Minjung Seo, Youngmi Kim, Jeong-Hun Sohn, Youngsam Park, Moon Kyeong Ju, Junghwan Kim, Sung-Jun Han, Tae-Hee Kim, Jonathan Cechetto, Jiyoun Nam, Peter Sommer, Zaesung No,