title: Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands.
abstract: A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H(4) receptor. Structure-activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H(4) receptor.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C. 3210 Merryfield Row, San Diego, CA 92121, USA. alee7@prdus.jnj.com <alee7@prdus.jnj.com>
authors.forename: Alice
authors.initials: A
authors.lastname: Lee-Dutra
authors.forename: Kristen L
authors.initials: KL
authors.lastname: Arienti
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: Buzard
authors.forename: Michael D
authors.initials: MD
authors.lastname: Hack
authors.forename: Haripada
authors.initials: H
authors.lastname: Khatuya
authors.forename: Pragnya J
authors.initials: PJ
authors.lastname: Desai
authors.forename: Steven
authors.initials: S
authors.lastname: Nguyen
authors.forename: Robin L
authors.initials: RL
authors.lastname: Thurmond
authors.forename: Lars
authors.initials: L
authors.lastname: Karlsson
authors.forename: James P
authors.initials: JP
authors.lastname: Edwards
authors.forename: J Guy
authors.initials: JG
authors.lastname: Breitenbucher
mesh_terms: D000447:Aldehydes / Q000737:chemistry; D000588:Amines / Q000737:chemistry; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D002384:Catalysis; D003198:Computer Simulation; D006632:Histamine / Q000378:metabolism; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000378:metabolism*; D011968:Receptors, Histamine / Q000737:chemistry / Q000378:metabolism*; D000074040:Receptors, Histamine H4; D013329:Structure-Activity Relationship
chemical_list: D000447:Aldehydes; D000588:Amines; D001562:Benzimidazoles; C418607:HRH4 protein, human; D008024:Ligands; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D000074040:Receptors, Histamine H4; D006632:Histamine