A novel 3,4-dihydropyrimidin-2(1H)-one: HIV-1 replication inhibitors with improved metabolic stability

DOI: 10.1016/j.bmcl.2012.01.133

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Bioorganic and Medicinal Chemistry Letters p. 2522 - 2526 (2012)

Update date:2022-08-06

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Authors:

Kim, Junwon

Ok, Taedong

Park, Changmin

So, Wonyoung

Jo, Mina

Kim, Youngmi

Seo, Minjung

Lee, Doohyun

Jo, Suyeon

Ko, Yoonae

Choi, Inhee

Park, Youngsam

Yoon, Jaewan

Ju, Moon Kyeong

Ahn, Jiye

Kim, Junghwan

Han, Sung-Jun

Kim, Tae-Hee

Cechetto, Jonathan

Nam, Jiyoun

Liuzzi, Michel

Sommer, Peter

No, Zaesung

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Article abstract of DOI:10.1016/j.bmcl.2012.01.133

Following the previous SAR of a novel dihydropyrimidinone scaffold as HIV-1 replication inhibitors a detailed study directed towards optimizing the metabolic stability of the ester functional group in the dihydropyrimidinone (DHPM) scaffold is described. Replacement of the ester moiety by thiazole ring significantly improved the metabolic stability while retaining antiviral activity against HIV-1 replication. These novel and potent DHPMs with bioisosteres could serve as advanced leads for further optimization.

Full text of DOI:10.1016/j.bmcl.2012.01.133

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