6801-22-5Relevant articles and documents
Exploiting the polypharmacology of ?-carbolines to disrupt o. volvulus molting
Gooyit, Major,Tricoche, Nancy,Javor, Sacha,Lustigman, Sara,Janda, Kim D.
supporting information, p. 339 - 343 (2015/03/30)
Onchocerciasis is an infection caused by the filarial worm Onchocerca volvulus, which can eventually result in blindness. The lack of an effective macrofilaricide and the possible development of ivermectin-resistant strains of O. volvulus necessitate the need for alternative treatment strategies. We have shown that targeting the L3-stage-specific chitinase OvCHT1 impairs the shedding of the filarial cuticle. In our continued efforts to discover OvCHT1 inhibitors, we identified the β-carboline alkaloid scaffolding as a chitinase inhibitor that is capable of penetrating the worm cuticle. Herein, we disclose the rich polypharmacology of the β-carboline class of compounds as an approach to abrogate the molting of the parasite and thus the initiation of infection in the human host.