358780-13-9Relevant articles and documents
3-Substituted Quinolines as RORγt Inverse Agonists
Tanis, Virginia M.,Venkatesan, Hariharan,Cummings, Maxwell D.,Albers, Michael,Kent Barbay,Herman, Krystal,Kummer, David A.,Milligan, Cynthia,Nelen, Marina I.,Nishimura, Rachel,Schlueter, Thomas,Scott, Brian,Spurlino, John,Wolin, Ronald,Woods, Craig,Xue, Xiaohua,Edwards, James P.,Fourie, Anne M.,Leonard, Kristi
, p. 1463 - 1470 (2019)
We have previously reported the syntheses of a series of 3,6-disubstituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma t (RORγt). These molecules are potent binders but are high molecular weight and they exhibited poor solubility at pH 2 and pH 7. This manuscript details our efforts at improving physical chemical properties for this series of compounds by increasing the diversity at the 3-position (i.e. introducing heteroatoms and lowering the molecular weight). These efforts have led to molecules which are potent binders with improved solubility.
Nickel-Catalyzed Addition of C–C Bonds of Amides to Strained Alkenes: The 1,2-Carboaminocarbonylation Reaction
Ito, Yuri,Kodama, Takuya,Nakatani, Syun,Shiraki, Ryota,Tobisu, Mamoru
supporting information, p. 662 - 666 (2022/02/05)
C(aryl)–C(═O) bonds of aryl amides can be activated and added across alkenes with the aid of a nickel catalyst. This 1,2-carboaminocarbonylation reaction enables the dicarbofunctionalization of alkenes with an atom economy of 100%.
Novel Inhibitors of an Insect Pest Chitinase: Design and Optimization of 9-O-Aromatic and Heterocyclic Esters of Berberine
Chen, Lei,Cheng, Jiagao,Qian, Xuhong,Shao, Xusheng,Yang, Qing,Zhu, Ling
, p. 7526 - 7533 (2021/07/26)
OfChi-h, a lepidopteran-exclusive glycoside hydrolase family 18 (GH18) chitinase from the agricultural insect pest Ostrinia furnacalis, is a promising molecular target candidate for pest control and management. Berberine (BER), a traditional Chinese medic