Synthesis and biological evaluation of novel N1-phenylsulphonyl indole derivatives as potent and selective 5-HT6R ligands for the treatment of cognitive disorders. (1st November 2016)

• Record Type: Journal Article
• Authors: Nirogi, Ramakrishna V. S.; Bandyala, Thrinath Reddy; Gangadasari, Pamuletinarasimha Reddy; Khagga, Mukkanti
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 31(2016 Feb.)Supplement 1
• Page Start: 1
• Page End: 15
• Publication Date: 2016-11-01
• Subjects: 5-Hydroxytryptamine-6 receptor -- animal models -- central nervous system -- cognition -- novel object recognition test -- structure–activity relationship; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2015.1103233
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: A series of 1-[3-(4-methyl piperazin-1-ylmethyl) phenylsulfonyl]-1 H -indole and 1-[3-(4-ethyl piperazin-1-ylmethyl) phenylsulfonyl]-1 H -indole derivatives were designed and synthesized as 5-HT6 receptor (5-HT6 R) ligands. The lead compound 1-[4-methyl-3-(4-methyl piperazin-1-yl methyl) phenylsulfonyl]-1 H -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.