title: 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
abstract: With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, a series of 2-(4-alkylpiperazin-1-yl)quinolines was prepared. Systematic variation of the substituents led to highly potent histamine H(3) antagonists with low polar surface area and appropriate log P for blood-brain barrier penetration.
authors.affiliation: Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark. flo@novonordisk.com
authors.forename: Florencio
authors.initials: F
authors.lastname: Zaragoza
authors.forename: Henrik
authors.initials: H
authors.lastname: Stephensen
authors.forename: Bernd
authors.initials: B
authors.lastname: Peschke
authors.forename: Karin
authors.initials: K
authors.lastname: Rimvall
mesh_terms: D000818:Animals; D001671:Biochemistry / Q000379:methods; D001812:Blood-Brain Barrier / Q000187:drug effects; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006633:Histamine Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D018100:Receptors, Histamine H3 / Q000187:drug effects* / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D006633:Histamine Antagonists; D007093:Imidazoles; D011804:Quinolines; D018100:Receptors, Histamine H3; D011985:Receptors, Serotonin