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Sovitj Pou; Rolf W. Winter; Aaron Nilsen; Jane Xu Kelly; Yuexin Li; J. Stone Doggett; Erin W. Riscoe; Keith W. Wegmann; David J. Hinrichs; Michael K. Riscoe (Profiled Author: Joseph Doggett)
Antimicrobial Agents and Chemotherapy. 2012;56(7):3475-3480.Abstract
Sontochin was the original chloroquine replacement drug, arising from research by Hans Andersag 2 years after chloroquine (known as "resochin" at the time) had been shelved due to the mistaken perception that it was too toxic for human use. We were surprised to find that sontochin, i.e., 3-methyl-chloroquine, retains significant activity against chloroquine-resistant strains of Plasmodium falciparum in vitro. We prepared derivatives of sontochin, "pharmachins," with alkyl or aryl substituents at the 3 position and with alterations to the 4-position side chain to enhance activity against drug-resistant strains. Modified with an aryl substituent in the 3 position of the 7-chloro-quinoline ring, Pharmachin 203 (PH-203) exhibits low-nanomolar 50% inhibitory concentrations (IC
PMID: 22508305 PMCID: PMC3393441
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