326595-66-8Relevant articles and documents
Discovery of novel quinazoline-2,4(1H,3H)-dione derivatives as potent PARP-2 selective inhibitors
Zhao, Hailong,Ji, Ming,Cui, Guonan,Zhou, Jie,Lai, Fangfang,Chen, Xiaoguang,Xu, Bailing
, p. 4045 - 4054 (2017)
The PARP-2 selective inhibitor is important for clarifying specific roles of PARP-2 in the pathophysiological process and developing desired drugs with reduced off-target side effects. In this work, a series of novel quinazoline-2,4(1H,3H)-dione derivatives was designed and synthesized to explore isoform selective PARP inhibitors. As a result, compound 11a (PARP-1 IC50?=?467?nM, PARP-2 IC50?=?11.5?nM, selectivity PARP-1/PARP-2?=?40.6) was disclosed as the most selective PARP-2 inhibitor with high potency to date. The binding features of compound 11a within PARP-1 and PARP-2 were investigated respectively to provide useful insights for the further construction of new isoform selective inhibitors of PARP-1 and PARP-2 by using CDOCKER program.
Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia
Yan, Yinfa,Zhou, Ping,Rotella, David P.,Feenstra, Rolf,Kruse, Chris G.,Reinders, Jan-Hendrik,Neut, Martina van der,Lai, Margaret,Zhang, Jean,Kowal, Dianne M.,Carrick, Tikva,Marquis, Karen L.,Pausch, Mark H.,Robichaud, Albert J.
scheme or table, p. 2983 - 2986 (2010/08/06)
A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D2 ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D2 partial agonists and serotonin reuptake inhibitors. Structure-activity studies revealed that the linker plays a key role in contributing to D2 affinity, function, and SRI activity.
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2′-amino-4′-substituted-phenylthio)benzylamines: Potential candidates as selective serotonin transporter radioligands
Jarkas, Nachwa,McConathy, Jonathan,Voll, Ronald J.,Goodman, Mark M.
, p. 4254 - 4265 (2007/10/03)
A series of N,N-dimethylated and N-monomethylated analogues of N,N-dimethyl-2-(2′-amino-4′-iodophenylthio)benzylamine substituted at the 4′-phenyl position have been prepared and evaluated in vitro for serotonin transporter (SERT) selectivity. Several der