Aryl-alkyl-lysines: small molecular membrane-active antiplasmodial agents.

Medchemcomm

Chemical biology and Medicinal Chemistry Laboratory , New Chemistry Unit , Jawaharlal Nehru Centre for Advanced Scientific Research (JNCASR), Jakkur , Bengaluru 560064 , Karnataka , India . Email:

Published: February 2017

Due to emerging resistance there is a steady need for new antimalarial drugs. Here, we report a new class of water soluble, non-toxic compounds, aryl-alkyl-lysines, with promising activity against the ring stage of . The optimal compound perturbed the plasma membrane potential and the digestive vacuole of parasites. In the murine model of malaria ( ANKA) the compound was able to increase the survival of mice by at least 5 days by an intra-peritoneal route. Further, the compounds showed no apparent toxicity to mice at the concentration tested.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6071861PMC
http://dx.doi.org/10.1039/c6md00589fDOI Listing

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