Publication | Open Access
Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents
101
Citations
7
References
2010
Year
Medicinal ChemistryAntimicrobial Drug DiscoveryCentral Linkage GroupsBiochemistryAntiparasitic AgentMedicineNatural SciencesParasitic ProtozoaBenzoxaborole Antitrypanosomal AgentsAntimicrobial ChemotherapyMicrobiologySulfur-linked SeriesDrug DevelopmentPharmacologyPharmaceutical ChemistryAntimicrobial ResistanceDrug 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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