title: N,N-Dimethyl-[9-(arylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]amines as novel, potent and selective 5-HT₆ receptor antagonists.
abstract: The design, synthesis and SAR of novel tetrahydrocarbazole derivatives having 5-HT(6) receptor antagonist activity is presented. The racemic compound 15e was found to possess desirable pharmacokinetic properties, adequate brain penetration and activity in animal models of cognition.
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India. ramakrishna_nirogi@yahoo.co.in
authors.forename: Ramakrishna V S
authors.initials: RV
authors.lastname: Nirogi
authors.forename: Jagadishu Babu
authors.initials: JB
authors.lastname: Konda
authors.forename: Ramasastry
authors.initials: R
authors.lastname: Kambhampati
authors.forename: Anil
authors.initials: A
authors.lastname: Shinde
authors.forename: Thrinath Reddy
authors.initials: TR
authors.lastname: Bandyala
authors.forename: Parandhama
authors.initials: P
authors.lastname: Gudla
authors.forename: Kiran Kumar
authors.initials: KK
authors.lastname: Kandukuri
authors.forename: Pradeep
authors.initials: P
authors.lastname: Jayarajan
authors.forename: Vishwottam
authors.initials: V
authors.lastname: Kandikere
authors.forename: P K
authors.initials: PK
authors.lastname: Dubey
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D001921:Brain / Q000378:metabolism; D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D006207:Half-Life; D006801:Humans; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000737:chemistry* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D000588:Amines; D002227:Carbazoles; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D013449:Sulfonamides; C097216:serotonin 6 receptor