37481-18-8Relevant articles and documents
Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays
Dang, Huong,Feichtinger, Konrad,Frazer, John,Grottick, Andrew J.,Kasem, Michelle,Le, Minh,Lehman, Juerg,Morgan, Michael E.,Ren, Albert,Sage, Carleton R.,Schrader, Thomas O.,Semple, Graeme,Unett, David J.,Whelan, Kevin T.,Wong, Amy,Zhu, Xiuwen
supporting information, (2020/01/22)
A series of potential new 5-HT2 receptor scaffolds based on a simplification of the clinically studied, 5-HT2CR agonist vabicaserin, were designed. An in vivo feeding assay early in our screening process played an instrumental part in the lead identification process, leading us to focus on a 6,5,7-tricyclic scaffold. A subsequent early SAR investigation provided potent agonists of the 5-HT2C receptor that were highly selective in both functional and binding assays, had good rat PK properties and that significantly reduced acute food intake in the rat.
Electrooxidative cyclization of hydroquinolyl alcohols, hydroquinolylamines, and dimethyl aminomalonates
Okimoto, Mitsuhiro,Yoshida, Takashi,Hoshi, Masayuki,Hattori, Kazuyuki,Komata, Masashi,Numata, Kaori,Tomozawa, Kenta
, p. 236 - 242 (2008/02/11)
Several hydroquinolyl alcohols and amines were electrochemically oxidized in methanol in the presence of sodium methoxide and potassium iodide to afford the corresponding intramolecular cyclization products. Furthermore, several amino malonates were electrochemically oxidized to yield the corresponding heterocyclic compounds through an intramolecular carbon-carbon bond formation in the presence of sodium cyanide in methanol. CSIRO 2007.