1312356-08-3Relevant academic research and scientific papers
1-Hydroxypyrido[2,3-d]pyrimidin-2(1H)-ones as novel selective HIV integrase inhibitors obtained via privileged substructure-based compound libraries
Gao, Ping,Zhang, Lingzi,Sun, Lin,Huang, Tianguang,Tan, Jing,Zhang, Jian,Zhou, Zhongxia,Zhao, Tong,Menéndez-Arias, Luis,Pannecouque, Christophe,Clercq, Erik De,Zhan, Peng,Liu, Xinyong
, p. 5779 - 5789 (2017/09/28)
A small library containing 3-hydroxyquinazoline-2,4(1H,3H)-dione and 1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one scaffolds was obtained via the copper(I)-catalyzed azidealkyne cycloaddition (CuAAC) reaction and evaluated for their anti-HIV activity in MT-4
4-(1,2,3-triazole substituted anilino)-pyridinopyrimidinones derivative and preparation method and application thereof
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Paragraph 0024; 0048; 0049; 0050; 0051, (2016/12/01)
The invention provides a 4-(1,2,3-triazole substituted anilino)-pyridinopyrimidinones derivative. The structure of the 4-(1,2,3-triazole substituted anilino)-pyridinopyrimidinones derivative is shown in the general formula I, wherein 1,2,3-triazole loop is aniline ortho-substituted and meta-substituted, and R is 4-fluorobenzyl or 4-methylbenzyl or phenethyl or phenylpropyl or 1-naphthyl or anilino acyl methyl or 4-fluoro- anilino acyl methyl or 4-fluoro-phenacyl or 4-trifluoromethyl-anilino acyl methyl. The invention further relates to a preparation method of the 4-(1,2,3-triazole substituted anilino)-pyridinopyrimidinones derivative and application of the 4-(1,2,3-triazole substituted anilino)-pyridinopyrimidinones derivative as an HIV inhibitor for preparing anti-AIDS medicine.
Pyridopyrimidinone inhibitors of HIV-1 RNase H
Velthuisen, Emile J.,Johns, Brian A.,Gerondelis, Peter,Chen, Yan,Li, Ming,Mou, Ke,Zhang, Wenwen,Seal, John W.,Hightower, Kendra E.,Miranda, Sonia R.,Brown, Kevin,Leesnitzer, Lisa
, p. 609 - 616 (2014/07/21)
Using a structure based pharmacophore design, a weak inhibitor of RNase H, identified from a small library of two metal binding HIV-1 integrase inhibitors, was optimized for potency and physicochemical properties. This manuscript describes the SAR and in vivo DMPK for the pyridopyrimidinone class of inhibitors.
