Organic Letters · 2015 · 63 citations · 7 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryMycologyStructure-activity RelationshipsChagas DiseaseLead Compound DesignLead DiscoveryNatural Product Drug DiscoveryProtozoal InfectionsProtozoan PathogenesisChemical DerivatizationDerivatizationEndophytic FungiEndophytic MicroorganismsMacrolide Antiparasitic AgentsNovel Antiparasitic Compound ClassesTreatment Of TrypanosomiasisTrypanosome Infections
Five new anti-trypanosomal macrolides, actinoallolides A-E (1-5), were discovered from the cultured broth of Actinoallomurus fulvus MK10-036. The structures of the actinoallolides, including absolute stereochemistry, were elucidated by a combination of spectroscopic analyses and a series of chemical derivatization studies. Actinoallolide A showed the most potent and selective in vitro anti-trypanosomal activity without cytotoxicity. A new class of promising lead compounds was identified for the development of drugs for both sleeping sickness and Chagas disease.
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Chagas disease: pushing through the pipeline
Julie Clayton · Nature · 2010 · 149 citations · Full text
Veterinary Medicine, Infectious Disease Control, Infectious Diseases +12