title: Indole- and benzothiophene-based histamine H3 antagonists.
abstract: Previous research on histamine H(3) antagonists has led to the development of a pharmacophore model consisting of a central phenyl core flanked by two alkylamine groups. Recent investigation of the replacement of the central phenyl core with heteroaromatic fragments resulted in the preparation of novel 3,5-, 3,6- and 3,7-substituted indole and 3,5-substituted benzothiophene analogs that demonstrate good to excellent hH(3) affinities. Select analogs were profiled in a rat pharmacokinetic model.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121-1126, United States.
authors.forename: Alejandro
authors.initials: A
authors.lastname: Santillan
authors.forename: Kelly J
authors.initials: KJ
authors.lastname: McClure
authors.forename: Brett D
authors.initials: BD
authors.lastname: Allison
authors.forename: Brian
authors.initials: B
authors.lastname: Lord
authors.forename: Jamin D
authors.initials: JD
authors.lastname: Boggs
authors.forename: Kirsten L
authors.initials: KL
authors.lastname: Morton
authors.forename: Anita M
authors.initials: AM
authors.lastname: Everson
authors.forename: Diane
authors.initials: D
authors.lastname: Nepomuceno
authors.forename: Michael A
authors.initials: MA
authors.lastname: Letavic
authors.forename: Alice
authors.initials: A
authors.lastname: Lee-Dutra
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
authors.forename: Cheryl A
authors.initials: CA
authors.lastname: Grice
mesh_terms: D000818:Animals; D051638:Ether-A-Go-Go Potassium Channels / Q000187:drug effects; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D007202:Indicators and Reagents; D007211:Indoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D007536:Isomerism; D008958:Models, Molecular; D051381:Rats; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D051638:Ether-A-Go-Go Potassium Channels; D054828:Histamine H3 Antagonists; D007202:Indicators and Reagents; D007211:Indoles; D013876:Thiophenes; C088015:benzothiophene