150004-57-2Relevant academic research and scientific papers
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment
Liu, Wenwen,Wang, Huan,Li, Xiaokang,Xu, Yixiang,Zhang, Jian,Wang, Wei,Gong, Qi,Qiu, Xiaoxia,Zhu, Jin,Mao, Fei,Zhang, Haiyan,Li, Jian
supporting information, p. 3117 - 3125 (2018/05/16)
Depression, a severe mental disease, is greatly difficult to treat and easy to induce other neuropsychiatric symptoms, the most frequent one is cognitive impairment. In this study, a series of novel vilazodone-tacrine hybrids were designed, synthesized and evaluated as multitarget agents against depression with cognitive impairment. Most compounds exhibited good multitarget activities and appropriate blood-brain barrier permeability. Specifically, compounds 1d and 2a exhibited excellent 5-HT1A agonist activities (1d, EC50 = 0.36 ± 0.08 nM; 2a, EC50 = 0.58 ± 0.14 nM) and 5-HT reuptake inhibitory activities (1d, IC50 = 20.42 ± 6.60 nM; 2a, IC50 = 22.10 ± 5.80 nM). In addition, they showed moderate ChE inhibitory activities (1d, AChE IC50 = 1.72 ± 0.217 μM, BuChE IC50 = 0.34 ± 0.03 μM; 2a, AChE IC50 = 2.36 ± 0.34 μM, BuChE IC50 = 0.10 ± 0.01 μM). Good multitarget activities with goodt blood-brain barrier permeability of 1d and 2a make them good lead compounds for the further study of depression with cognitive impairment.
QUINAZOLINONE AND PYRIDOPYRIMIDINE A-II ANTAGONISTS
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, (2008/06/13)
Substituted quinazolinones and pyridopyrimidines of structural formula 1 STR1 are angiotensin II antagonists useful in the treatment of disorders related to the reninangiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.
QUINAZOLINONES AND PYRIDOPYRIMIDINONES
-
, (2008/06/13)
Substituted quinazolinones and pyridopyrimidines of structural formula I STR1 are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.
