title: Novel small molecule bradykinin B1 receptor antagonists. Part 2: 5-membered diaminoheterocycles.
abstract: Efforts to find new bradykinin B(1) receptor antagonists identified 2-aminobenzimidazole as a novel core. Subsequent transformation into five-membered diaminoheterocycle derivatives and their synthesis and SAR is described. This resulted in compounds with low nanomolar activity.
authors.affiliation: Jerini AG, Invalidenstrasse 130, 10115 Berlin, Germany.
authors.forename: Gunther
authors.initials: G
authors.lastname: Zischinsky
authors.forename: Roland
authors.initials: R
authors.lastname: Stragies
authors.forename: Marco
authors.initials: M
authors.lastname: Schaudt
authors.forename: Jochen R
authors.initials: JR
authors.lastname: Pfeifer
authors.forename: Christoph
authors.initials: C
authors.lastname: Gibson
authors.forename: Elsa
authors.initials: E
authors.lastname: Locardi
authors.forename: Dirk
authors.initials: D
authors.lastname: Scharn
authors.forename: Uwe
authors.initials: U
authors.lastname: Richter
authors.forename: Holger
authors.initials: H
authors.lastname: Kalkhof
authors.forename: Klaus
authors.initials: K
authors.lastname: Dinkel
authors.forename: Karsten
authors.initials: K
authors.lastname: Schnatbaum
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D065169:Bradykinin B1 Receptor Antagonists; D002460:Cell Line; D003959:Diamines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D005347:Fibroblasts / Q000187:drug effects / Q000378:metabolism; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D043783:Receptor, Bradykinin B1 / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D065169:Bradykinin B1 Receptor Antagonists; D003959:Diamines; D006571:Heterocyclic Compounds; D043783:Receptor, Bradykinin B1; C027391:2-aminobenzimidazole