ACS Medicinal Chemistry Letters · 2010 · 102 citations · 7 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryStructure-activity RelationshipsAntiparasitic AgentsEnzyme InhibitionStructure-activity Relationship AnalysisAntiparasitic Drug DiscoveryAntitrypanosomal TherapyChemical Structure-activity RelationshipsIn Vivo Efficacy TestingMurine ModelsNovel Antiparasitic Compound ClassesNovel Antiparasitic Discovery
We report the discovery of benzoxaborole antitrypanosomal agents and their structure-activity relationships on central linkage groups and different substitution patterns in the sulfur-linked series. The compounds showed in vitro growth inhibition IC50 values as low as 0.02 μg/mL and in vivo efficacy in acute murine infection models against Tryapnosoma brucei.
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An Antifungal Agent Inhibits an Aminoacyl-tRNA Synthetase by Trapping tRNA in the Editing Site
Fernando Rock, Weimin Mao, A. Yaremchuk et al. · Science · 2007 · 631 citations · Full text
Tsutomu Akama, Stephen J. Baker, Yongkang Zhang et al. · Bioorganic & Medicinal Chemistry Letters · 2009 · 210 citations · Full text