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  • Title: Synthesis and Evaluation of Chirally Defined Side Chain Variants of 7-Chloro-4-Aminoquinoline To Overcome Drug Resistance in Malaria Chemotherapy.
    Author: Dola VR, Soni A, Agarwal P, Ahmad H, Raju KS, Rashid M, Wahajuddin M, Srivastava K, Haq W, Dwivedi AK, Puri SK, Katti SB.
    Journal: Antimicrob Agents Chemother; 2017 Mar; 61(3):. PubMed ID: 27956423.
    Abstract:
    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.
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