Identification of an orally active carbazole aminoalcohol derivative with broad-spectrum anti-animal trypanosomiasis activity

Oral Delivery of Anti-Parasitic Agent-Loaded PLGA Nanoparticles: Enhanced Liver Targeting and Improved Therapeutic Effect on Hepatic Alveolar Echinococcosis

“…Carbazole alkaloid, as a privileged structure in medicinal chemistry, has been widely reported to have extensive biological activities including antimicrobial, antitumor, antiviral and anti-Alzheimer. [28][29][30][31] In the previous studies, we designed and synthesized a series of carbazole aminoalcohol derivatives (one representative is H1402), which exhibited broad-spectrum anti-parasitic activities against Echinococcus and Trypanozoon in vitro and in vivo, 15,16,32 and Plasmodium and Schistosoma in vitro. 33 Especially significant therapeutic efficacy was achieved following the oral treatments of the carbazole aminoalcohols in mice infected with E. granulosus s.l., while unfortunately the anti-parasitic potency declined for AE.…”