65625-49-2Relevant academic research and scientific papers
A recyclable and highly stereoselective multi-fluorous proline catalyst for asymmetric aldol reactions
Gotoh, Machiko,Ishihara, Kazuki,Ishihara, Kotaro,Kobayashi, Yuki,Matsugi, Masato,Obayashi, Riho,Shioiri, Takayuki,Watanabe, Yuki
supporting information, (2020/02/13)
A recyclable fluorous proline catalyst with high stereoselectivity that functions as a catalyst for asymmetric aldol reactions is described. Its high stereoselectivity and facile recovery are achieved by employing a multi-fluorous tag attachment strategy. Although a gradual decrease was observed with respect to the catalytic activity, the catalyst can be separated from the reaction mixture by adsorption onto FluoroFlash and can be reused in that form for a maximum of five times while maintaining a high stereoselectivity.2019 Elsevier Ltd. All rights reserved.
Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays
Huang, Boshi,Wang, Xueshun,Liu, Xinhao,Chen, Zihui,Li, Wanzhuo,Sun, Songkai,Liu, Huiqing,Daelemans, Dirk,De Clercq, Erik,Pannecouque, Christophe,Zhan, Peng,Liu, Xinyong
, p. 4397 - 4406 (2017/07/22)
Crystallographic overlap studies and pharmacophoric analysis indicated that diarylpyrimidine (DAPY)-based HIV-1 NNRTIs showed a similar binding mode and pharmacophoric features as indolylarylsulfones (IASs), another class of potent NNRTIs. Thus, a novel series of DAPY-IAS hybrid derivatives were identified as newer NNRTIs using structure-based molecular hybridization. Some target compounds exhibited moderate activities against HIV-1 IIIB strain, among which the two most potent inhibitors possessed EC50 values of 1.48?μM and 1.61?μM, respectively. They were much potent than the reference drug ddI (EC50?=?76.0?μM) and comparable to 3TC (EC50?=?2.54?μM). Compound 7a also exhibited the favorable selectivity index (SI?=?80). Preliminary structure-activity relationships (SARs), structure-cytotoxicity relationships, molecular modeling studies, and in silico calculation of physicochemical properties of these new inhibitors were also discussed.
