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Journal articles
Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication.
Junwon Kim
1
Changmin Park
1
Taedong Ok
1
Wonyoung So
1
Mina Jo
1
Minjung Seo
1
Youngmi Kim
1
Jeong-Hun Sohn
1
Youngsam Park
1
Moon Kyeong Ju
1
Junghwan Kim
1
Sung-Jun Han
1
Tae-Hee Kim
1
Jonathan Cechetto
1
Jiyoun Nam
1
Peter Sommer
1
Zaesung No
1, *
*
Corresponding author
Zaesung No 1
Correspondent author
1
Institut Pasteur Korea - Institut Pasteur de Corée (39-1, Hawolgok-dong, Sungbuk-gu, Seoul 136-791 - South Korea)
- RIIP - Réseau International des Instituts Pasteur (25, rue du Dr Roux 75724 Paris Cedex 15 - France)
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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https://hal-riip.archives-ouvertes.fr/pasteur-00683848
Contributor : Peter Sommer <>
Submitted on : Friday, March 30, 2012 - 5:34:17 AM
Last modification on : Wednesday, September 23, 2020 - 10:44:03 AM
Long-term archiving on: : Wednesday, December 14, 2016 - 6:46:58 PM
Contributor : Peter Sommer <>
Submitted on : Friday, March 30, 2012 - 5:34:17 AM
Last modification on : Wednesday, September 23, 2020 - 10:44:03 AM
Long-term archiving on: : Wednesday, December 14, 2016 - 6:46:58 PM
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- HAL Id : pasteur-00683848, version 1
- DOI : 10.1016/j.bmcl.2011.12.090
- PUBMED : 22305583
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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⟩
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