1224680-65-2Relevant academic research and scientific papers
A novel 3,4-dihydropyrimidin-2(1H)-one: HIV-1 replication inhibitors with improved metabolic stability
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
scheme or table, p. 2522 - 2526 (2012/05/05)
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.
ANTI VIRAL COMPOUNDS
-
Page/Page column 52-53, (2010/05/13)
There is provided small molecule anti-human immunodeficiency virus (anti-HIV) compounds as well as a phenotypic cell-based high throughput screening (HTS) assay for their identification.
