title: Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists).
abstract: A series of novel benzimidazole derivatives has been designed via a scaffold morphing approach based on known calcilytics chemotypes. Subsequent lead optimisation led to the discovery of penta-substituted benzimidazoles that exhibit attractive in vitro and in vivo calcium-sensing receptor (CaSR) inhibitory profiles. In addition, synthesis and structure-activity relationship data are provided.
authors.affiliation: Novartis Institutes for BioMedical Research, Novartis Pharma AG, Basel, Switzerland. marc.gerspacher@novartis.com
authors.forename: Marc
authors.initials: M
authors.lastname: Gerspacher
authors.forename: Eva
authors.initials: E
authors.lastname: Altmann
authors.forename: René
authors.initials: R
authors.lastname: Beerli
authors.forename: Thomas
authors.initials: T
authors.lastname: Buhl
authors.forename: Ralf
authors.initials: R
authors.lastname: Endres
authors.forename: Rainer
authors.initials: R
authors.lastname: Gamse
authors.forename: Jacques
authors.initials: J
authors.lastname: Kameni-Tcheudji
authors.forename: Michaela
authors.initials: M
authors.lastname: Kneissel
authors.forename: Karl Heinz
authors.initials: KH
authors.lastname: Krawinkler
authors.forename: Martin
authors.initials: M
authors.lastname: Missbach
authors.forename: Alfred
authors.initials: A
authors.lastname: Schmidt
authors.forename: Klaus
authors.initials: K
authors.lastname: Seuwen
authors.forename: Sven
authors.initials: S
authors.lastname: Weiler
authors.forename: Leo
authors.initials: L
authors.lastname: Widler
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D008958:Models, Molecular; D044169:Receptors, Calcium-Sensing / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D044169:Receptors, Calcium-Sensing