Antimicrobial Agents and Chemotherapy (2017)
Update date:2022-08-15
Topics:
Dola, Vasantha Rao
Soni, Awakash
Agarwal, Pooja
Ahmad, Hafsa
Raju, Kanumuri Siva Rama
Rashid, Mamunur
Wahajuddin, Muhammad
Srivastava, Kumkum
Haq
Dwivedi
Puri
Katti
A novel 4-aminoquinoline derivative [(S)-7-chloro-N-(4-methyl-1-(4-methyl-piperazin-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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Doi:10.1039/c2ob00015f
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