Synthesis and Evaluation of Chirally Defined Side Chain Variants of 7-Chloro4-Aminoquinoline To Overcome Drug Resistance in Malaria Chemotherapy

被引：0

作者：

Dola, Vasantha Rao ^{[1
]}

Soni, Awakash ^{[2
]}

Agarwal, Pooja ^{[2
]}

Ahmad, Hafsa ^{[3
]}

Raju, Kanumuri Siva Rama ^{[4
]}

Rashid, Mamunur ^{[4
]}

Wahajuddin, Muhammad ^{[4
]}

Srivastava, Kumkum ^{[2
]}

Haq, W. ^{[1
]}

Dwivedi, A. K. ^{[3
]}

Puri, S. K. ^{[2
]}

Katti, S. B. ^{[1
]}

机构：

[1] Cent Drug Res Inst, Div Med & Proc Chem, Lucknow, Uttar Pradesh, India

[2] Cent Drug Res Inst, Parasitol, Lucknow, Uttar Pradesh, India

[3] Cent Drug Res Inst, Pharmaceut, Lucknow, Uttar Pradesh, India

[4] Cent Drug Res Inst, Pharmacokinet & Metab, Lucknow, Uttar Pradesh, India

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2017年 / 61卷 / 03期

关键词：

4-aminoquinoline; antimalarial agents; chloroquine resistant; quinolines; HEME POLYMERIZATION INHIBITION; PLASMODIUM-FALCIPARUM; ANTIMALARIAL ACTIVITY; IN-VITRO; 4-AMINOQUINOLINE DERIVATIVES; ANTIPLASMODIAL ACTIVITY; RETAIN ACTIVITY; CHLOROQUINE; ANALOGS; DESIGN;

D O I：

10.1128/AAC.01152-16

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

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.

引用

页数：26

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