744219-30-5Relevant academic research and scientific papers
Novel inhibitors of nicotinamide-n-methyltransferase for the treatment of metabolic disorders
Czech, Joerg,Dhakshinamoorthy, Saravanakumar,Hallur, Mahanandeesha S.,Kannt, Aimo,Kristam, Rajendra,Rajagopal, Sridharan,Ruf, Sven,Schreuder, Herman,Swamy, Indu,Zech, Gernot
supporting information, (2021/06/12)
Nicotinamide-N-methyltransferase (NNMT) is a cytosolic enzyme catalyzing the transfer of a methyl group from S-adenosyl-methionine (SAM) to nicotinamide (Nam). It is expressed in many tissues including the liver, adipose tissue, and skeletal muscle. Its expression in several cancer cell lines has been widely discussed in the literature, and recent work established a link between NNMT expression and metabolic diseases. Here we describe our approach to identify potent small molecule inhibitors of NNMT featuring different binding modes as elucidated by X-ray crystallographic studies.
An improved synthesis of 4-(1-Piperazinyl)benzo[ b ]thiophene Dihydrochloride
Wu, Chunhui,Chen, Weiming,Jiang, Dehui,Jiang, Xiangrui,Shen, Jingshan
, p. 555 - 558 (2015/04/27)
2-Chloro-6-fluorobenzaldehyde was converted to 4-(1-piperazinyl)benzo[b]thiophene dihydrochloride (18), an intermediate in the synthesis of brexpiprazole, via a five-step sequence in 54% overall yield. This procedure requires no expensive catalyst and avoids the side products produced in the coupling step in the reported process. Several kilograms of compound 18 were prepared using this economical and scalable process.
5-piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists
Liu, Kevin G.,Robichaud, Albert J.,Bernotas, Ronald C.,Yan, Yinfa,Lo, Jennifer R.,Zhang, Mei-Yi,Hughes, Zoe A.,Huselton, Christine,Zhang, Guo Ming,Zhang, Jean Y.,Kowal, Dianne M.,Smith, Deborah L.,Schechter, Lee E.,Comery, Thomas A.
scheme or table, p. 7639 - 7646 (2011/02/21)
As part of our efforts to develop agents for CNS diseases, we have been focused on the 5-HT6 receptor in order to identify potent and selective ligands for cognitive enhancement. Herein we report the identification of a novel series of 5-piperazinyl-3-sulfonylindazoles as potent and selective 5-HT6 antagonists. The synthesis, SAR, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole (WAY-255315 or SAM-315) will be described.
Heterocyclyl-3-sulfonylindazoles as 5-hydroxytryptamine-6 ligands
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Page/Page column 19, (2008/06/13)
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
