43171-49-9Relevant articles and documents
Substituent Position-Controlled Stereoselectivity in Enzymatic Reduction of Diaryl- and Aryl(heteroaryl)methanones
Li, Zhining,Wang, Zexu,Wang, Yuhan,Wu, Xiaofan,Lu, Hong,Huang, Zedu,Chen, Fener
supporting information, p. 1859 - 1865 (2019/03/07)
We report here the discovery of a novel ketoreductase (KRED), named KmCR2, with a broad substrate spectrum on bioreduction of sterically bulky diaryl- and aryl(heteroaryl)methanones. The position of the substituent on aromatic rings (meta versus para or ortho) was revealed to control the stereospecificity of KmCR2. The stereoselective preparation of both enantiomers of diaryl- or aryl(heteroaryl)methanols using strategically engineered substrates with a traceless directing group (bromo group) showcased the potential application of this substrate-controlled bioreduction reaction. The combined use of substrate engineering and protein engineering, was demonstrated to be a useful strategy in efficiently improving stereoselectivity or switching stereopreference of enzymatic processes. (Figure presented.).
Synthesis and anticonvulsant activity of some cinnamylpiperazine derivatives
Hu, Chuan,Sun, Zhi-Gang,Wei, Cheng-Xi,Quan, Zhe-Shan
scheme or table, p. 661 - 664 (2011/11/29)
A series of cinnamylpiperazine derivatives was synthesized using different benzophenone as starting material. The structures of the compounds were proved by their IR, 1H-NMR spectroscopic data and mass spectra data. The anticonvulsant activities of these compounds were evaluated with maximal electroshock (MES) test and rotarod test with intraperitoneal injection on KunMing mice. Among all the flunarizine analogues, no one exhibited better anticonvulsant activity than flunarizine. Flunarizine (4i) exhibited anticonvulsant activity with ED50 of 38.1 mg/kg, TD50 of 164.3 mg/kg and PI of 4.3 through administration intraperitoneal, and with ED50 of 56.8 mg/kg, TD50 of 456.3 mg/kg and PI of 8.0 through oral administration.
Convenient synthesis of structurally novel 1,3-disubstituted azetidine derivatives
Kharul, Rajendra K.,Goswami, Amitgiri,Gite, Archana,Godha, Atul K.,Jain, Mukul,Patel, Pankaj R.
, p. 1703 - 1717 (2008/09/20)
A convenient synthesis of structurally novel 1,3-disubstituted azetidine derivatives is described. The approach involves condensation of an azetidine building block with sulfonylated carbamic acid methyl ester, subsequently followed by quenching the imidoyl chloride with amines. Different derivatives were prepared by substituting benzhydrol as well as benzenesulfonamide as part of the core structure. Copyright Taylor & Francis Group, LLC.