Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication |
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| Authors: | Kim Junwon Park Changmin Ok Taedong So Wonyoung Jo Mina Seo Minjung Kim Youngmi Sohn Jeong-Hun Park Youngsam Ju Moon Kyeong Kim Junghwan Han Sung-Jun Kim Tae-Hee Cechetto Jonathan Nam Jiyoun Sommer Peter No Zaesung |
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| Institution: | Medicinal Chemistry Group, Institut Pasteur Korea (IP-K), Sampyeong-dong 696, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea. |
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| 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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