473596-87-1Relevant articles and documents
Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores
Liu, Jian,Shao, Patrick P.,Guiadeen, Deodial,Krikorian, Arto,Sun, Wanying,Deng, Qiaolin,Cumiskey, Anne-Marie,Duffy, Ruth A.,Murphy, Beth A.,Mitra, Kaushik,Johns, Douglas G.,Duffy, Joseph L.,Vachal, Petr
, (2020/11/18)
Cholesteryl ester transfer protein (CETP) inhibitors reduce the transfer of cholesteryl esters from the high-density lipoprotein (HDL-C) to apolipoprotein such as VLDL/LDL, with exchange of triglycerides. Thus, this inhibition increases the HDL-C levels, which is believed to lower the risk for heart disease and stroke. We report here a series of CETP inhibitors based on the cyclic, bicyclic urea and sulfamide cores. These CETP inhibitors exemplified by 15, 31, and 45 demonstrated in vitro potency in inhibiting the CETP transfer activity, and 15, 31 showing in vivo efficacy to increase HDL-C levels in cynomolgus-CETP transgenic mice. The synthesis and biological evaluations of these CETP inhibitors are described.
Visible-light-mediated borylation of aryl and alkyl halides with a palladium complex
Zhao, Jia-Hui,Zhou, Zhao-Zhao,Zhang, Yue,Su, Xuan,Chen, Xi-Meng,Liang, Yong-Min
supporting information, p. 4390 - 4394 (2020/10/20)
Palladium catalyzed visible-light-mediated borylation of inactivated aryl and alkyl halides is reported; the method provided high yields and excellent functional group compatibility. Furthermore, arylsilicates were synthesized selectively using dimethylphenylsilyl boronic ester via changing the reaction conditions. Finally, the possible reaction mechanism is determined through fluorescence quenching and turn on/off experiments.
Reversible Covalent End-Capping of Collagen Model Peptides
Priem, Christoph,Geyer, Armin
supporting information, p. 14278 - 14283 (2019/11/03)
The combination of supramolecular aggregation of collagen model peptides with reversible covalent end-capping of the formed triple helix in a single experimental set-up yielded minicollagens, which were characterized by a single melting temperature. In spite of the numerous possible reaction intermediates, a specific synthetic collagen with a leading, middle and trailing strand is formed in a highly cooperative self-assembly process.