کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10593834 | 981813 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 5, 1 March 2012, Pages 2119-2124
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 5, 1 March 2012, Pages 2119-2124
نویسندگان
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,