Synthesis and evaluation of novel bacterial rRNA-binding benzimidazoles by mass spectrometry.
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.
He
Yun
Y
Ibis Therapeutics, A Division of Isis Pharmaceuticals, Inc, 2292 Faraday Av, Carlsbad, CA 92008, USA. yhe@gnf.org
Yang
Jun
J
Wu
Baogen
B
Robinson
Dale
D
Sprankle
Kelly
K
Kung
Pei-Pei
PP
Lowery
Kristin
K
Mohan
V
V
Hofstadler
Steve
S
Swayze
Eric E
EE
Griffey
Rich
R
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
D001562:Benzimidazoles; D012329:RNA, Bacterial; D012336:RNA, Ribosomal, 16S