A Divergent Synthesis of Numerous Pyrroloiminoquinone Alkaloids Identifies Promising Antiprotozoal Agents
Barnes G, Magann N, Perrotta D, Hörmann F, Fernandez S, Vydyam P, Choi J, Prudhomme J, Neal A, Le Roch K, Mamoun C, Vanderwal C. A Divergent Synthesis of Numerous Pyrroloiminoquinone Alkaloids Identifies Promising Antiprotozoal Agents. Journal Of The American Chemical Society 2024, 146: 29883-29894. PMID: 39412402, PMCID: PMC11528414, DOI: 10.1021/jacs.4c11897.Peer-Reviewed Original ResearchNatural productsLarock indole synthesisAlkaloid natural productsAmine nucleophilesDivergent synthesisIndole synthesisPyrrolic nitrogenMethoxy groupLead compoundsDrug discoveryCompoundsStructural analogsPlasmodium falciparum</i>SynthesisPyrroloiminoquinoneHuman cytotoxicityMalaria parasitesNucleophilesPyrroleAntiprotozoal agentsAminesMammalian cellsIntermediateIn vitro efficacy of next-generation dihydrotriazines and biguanides against babesiosis and malaria parasites
Vydyam P, Chand M, Gihaz S, Renard I, Heffernan G, Jacobus L, Jacobus D, Saionz K, Shah R, Shieh H, Terpinski J, Zhao W, Cornillot E, Mamoun C. In vitro efficacy of next-generation dihydrotriazines and biguanides against babesiosis and malaria parasites. Antimicrobial Agents And Chemotherapy 2024, 68: e00423-24. PMID: 39136469, PMCID: PMC11373198, DOI: 10.1128/aac.00423-24.Peer-Reviewed Original ResearchTherapeutic indexPlasmodium falciparum</i>Effective therapeutic strategyCausative agent of babesiosisIn vitro efficacyAntiparasitic drugsProtozoan parasitesMalaria parasitesIntraerythrocytic protozoan parasiteTherapeutic strategiesFolate pathwayBroad-spectrum antiparasitic drugStrain HB3Babesia divergensMalariaBabesia duncaniAnimal healthAntifolatesDrugWidespread resistanceCausative agentBiguanideBabesiaBabesiosisBiosynthesis of purines