title: Synthesis and evaluation of novel bacterial rRNA-binding benzimidazoles by mass spectrometry.
abstract: A series of novel benzimidazoles were efficiently synthesized using both solution- and solid-phase chemistry. These compounds were found to bind to the bacterial 16S ribosomal RNA A-site with micromolar affinities using unique mass spectrometry-based assays.
authors.affiliation: Ibis Therapeutics, A Division of Isis Pharmaceuticals, Inc, 2292 Faraday Av, Carlsbad, CA 92008, USA. yhe@gnf.org
authors.forename: Yun
authors.initials: Y
authors.lastname: He
authors.forename: Jun
authors.initials: J
authors.lastname: Yang
authors.forename: Baogen
authors.initials: B
authors.lastname: Wu
authors.forename: Dale
authors.initials: D
authors.lastname: Robinson
authors.forename: Kelly
authors.initials: K
authors.lastname: Sprankle
authors.forename: Pei-Pei
authors.initials: PP
authors.lastname: Kung
authors.forename: Kristin
authors.initials: K
authors.lastname: Lowery
authors.forename: V
authors.initials: V
authors.lastname: Mohan
authors.forename: Steve
authors.initials: S
authors.lastname: Hofstadler
authors.forename: Eric E
authors.initials: EE
authors.lastname: Swayze
authors.forename: Rich
authors.initials: R
authors.lastname: Griffey
mesh_terms: D020029:Base Pairing; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D001665:Binding Sites; D004926:Escherichia coli; D013058:Mass Spectrometry; D008958:Models, Molecular; D009690:Nucleic Acid Conformation; D012329:RNA, Bacterial / Q000737:chemistry / Q000378:metabolism*; D012336:RNA, Ribosomal, 16S / Q000737:chemistry / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D012329:RNA, Bacterial; D012336:RNA, Ribosomal, 16S