Synthesis and biological evaluation of novel N1-phenylsulphonyl indole derivatives as potent and selective 5-HT6R ligands for the treatment of cognitive disorders

被引:2
作者
Nirogi, Ramakrishna V. S. [1 ]
Bandyala, Thrinath Reddy [1 ,2 ]
Gangadasari, Pamuletinarasimha Reddy [1 ]
Khagga, Mukkanti [2 ]
机构
[1] Suven Life Sci Ltd, Discovery Res, Rd 5,Ave 7, Hyderabad 500034, Andhra Pradesh, India
[2] Jawaharlal Nehru Technol Univ Hyderabad, Inst Sci & Technol, Ctr Chem Sci & Technol, Hyderabad, Andhra Pradesh, India
关键词
5-Hydroxytryptamine-6; receptor; animal models; central nervous system; cognition; novel object recognition test; structure-activity relationship; PHARMACOLOGICAL EVALUATION; RECEPTOR ANTAGONISTS; SEROTONIN; BINDING; RAT; SB-271046; SYMPTOMS; CORTEX;
D O I
10.3109/14756366.2015.1103233
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of 1-[3-(4-methyl piperazin-1-ylmethyl) phenylsulfonyl]-1H-indole and 1-[3-(4-ethyl piperazin-1-ylmethyl) phenylsulfonyl]-1H-indole derivatives were designed and synthesized as 5-HT6 receptor (5-HT6R) ligands. The lead compound 1-[4-methyl-3-(4-methyl piperazin-1-yl methyl) phenylsulfonyl]-1H-indole dihydrochloride (6b), in this series, has shown potent in vitro binding affinity, selectivity, good pharmacokinetics (PK) profile and activity in the animal models of cognition.
引用
收藏
页码:1 / 15
页数:15
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