Antimicrobial Agents and Chemotherapy
Antimicrobial Agents and Chemotherapy
4 years ago

Synthesis and Evaluation of Chirally Defined Side Chain Variants of 7-Chloro-4-Aminoquinoline To Overcome Drug Resistance in Malaria Chemotherapy.

Srivastava K, Ahmad H, Dola VR, Agarwal P, Puri SK, Katti SB, Dwivedi AK, Wahajuddin M, Soni A, Rashid M, Raju KS, Haq W
A novel 4-aminoquinoline derivative [(S)-7-chloro-N-(4-methyl-1-(4-methylpiperazin-1-yl)pentan-2-yl)-quinolin-4-amine triphosphate] exhibiting curative activity against chloroquine-resistant malaria parasites has been identified for preclinical development as a blood schizonticidal agent. The lead molecule selected after detailed structure-activity relationship (SAR) studies has good solid-state properties and promising activity against in vitro and in vivo experimental malaria models. The in vitro absorption, distribution, metabolism, and excretion (ADME) parameters indicate a favorable drug-like profile.

Publisher URL: https://www.ncbi.nlm.nih.gov/pubmed/27956423

DOI: PubMed:27956423

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