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

Vasantha Rao Dola | Zendy; Awakash Soni | Zendy; Pooja Agarwal | Zendy; Hafsa Ahmad | Zendy; Raju S. Kanumuri | Zendy; Mamunur Rashid | Zendy; Muhammad Wahajuddin | Zendy; Kumkum Srivastava | Zendy; W. Haq | Zendy; Anil Kumar Dwivedi | Zendy; S.K. Puri | Zendy; S. B. Katti | Zendy

Open Access

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

Author(s) -

Vasantha Rao Dola,

Awakash Soni,

Pooja Agarwal,

Hafsa Ahmad,

Raju S. Kanumuri,

Mamunur Rashid,

Muhammad Wahajuddin,

Kumkum Srivastava,

W. Haq,

Anil Kumar Dwivedi,

S.K. Puri,

S. B. Katti

Publication year - 2016

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.01152-16

Subject(s) - adme , malaria , pharmacology , in vivo , chloroquine , drug , plasmodium falciparum , in vitro , drug resistance , absorption (acoustics) , chemotherapy , chemistry , pharmacokinetics , excretion , medicine , biology , biochemistry , microbiology and biotechnology , immunology , materials science , composite material

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 againstin vitro andin vivo experimental malaria models. Thein vitro absorption, distribution, metabolism, and excretion (ADME) parameters indicate a favorable drug-like profile.

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