Ontology highlight
ABSTRACT:
SUBMITTER: Caglic D
PROVIDER: S-EPMC3983388 | biostudies-literature | 2014 Feb
REPOSITORIES: biostudies-literature
Caglič Dejan D Krutein Michelle C MC Bompiani Kristin M KM Barlow Deborah J DJ Benoni Galit G Pelletier Jeffrey C JC Reitz Allen B AB Lairson Luke L LL Houseknecht Karen L KL Smith Garry R GR Dickerson Tobin J TJ
Journal of medicinal chemistry 20140115 3
Botulinum neurotoxins (BoNT) are the most potent toxins known and a significant bioterrorist threat. Few small molecule compounds have been identified that are active in cell-based or animal models, potentially due to toxin enzyme plasticity. Here we screened commercially available quinolinols, as well as synthesized hydroxyquinolines. Seventy-two compounds had IC50 values below 10 μM, with the best compound exhibiting submicromolar inhibition (IC50 = 0.8 μM). Structure-activity relationship tre ...[more]