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本文引用的文献

1
A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold.一项发散性的构效关系研究使得一种强效5-HT2c抑制剂优化为一种有前景的抗疟骨架。
ACS Med Chem Lett. 2012 Feb 9;3(5):373-7. doi: 10.1021/ml300008j. eCollection 2012 May 10.
2
Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS).环丙基甲酰胺：源自特雷斯坎托斯抗疟药库（TCAMS）的新型口服抗疟药系列。
ACS Med Chem Lett. 2011 Aug 29;2(11):840-4. doi: 10.1021/ml2001517. eCollection 2011 Nov 10.
3
An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMS.疟疾药物研发中的开放式创新邀请：来自TCAMS的47个优质起点
ACS Med Chem Lett. 2011 Aug 3;2(10):741-6. doi: 10.1021/ml200135p. eCollection 2011 Oct 13.
4
A new in vivo screening paradigm to accelerate antimalarial drug discovery.一种新的体内筛选范式，加速抗疟药物发现。
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Assignment of the absolute configuration of polyfunctional compounds by NMR using chiral derivatizing agents.使用手性衍生试剂通过核磁共振确定多官能化合物的绝对构型
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P. falciparum in vitro killing rates allow to discriminate between different antimalarial mode-of-action.体外疟原虫杀伤率可用于区分不同的抗疟作用模式。
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Challenges in antimalarial drug discovery.抗疟药物研发的挑战。
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8
A randomized, double-blind, placebo-controlled study to investigate the safety, tolerability, and pharmacokinetics of single enantiomer (+)-mefloquine compared with racemic mefloquine in healthy persons.一项随机、双盲、安慰剂对照研究，旨在调查单一对映体 (+)-甲氟喹与消旋甲氟喹在健康人群中的安全性、耐受性和药代动力学。
Am J Trop Med Hyg. 2010 Dec;83(6):1195-201. doi: 10.4269/ajtmh.2010.10-0228.
9
Thousands of chemical starting points for antimalarial lead identification.数以千计的抗疟药物先导化合物化学起始点。
Nature. 2010 May 20;465(7296):305-10. doi: 10.1038/nature09107.
10
Artemisinin resistance in Plasmodium falciparum malaria.恶性疟原虫疟疾中的青蒿素耐药性。
N Engl J Med. 2009 Jul 30;361(5):455-67. doi: 10.1056/NEJMoa0808859.

小分子抗疟药的案例研究：2-氨基-1-苯乙醇（APE）衍生物

Case Study of Small Molecules As Antimalarials: 2-Amino-1-phenylethanol (APE) Derivatives.

作者信息

Chaparro María J, Vidal Jaume, Angulo-Barturen Iñigo, Bueno José M, Burrows Jeremy, Cammack Nicholas, Castañeda Pablo, Colmenarejo Gonzalo, Coterón José M, de Las Heras Laura, Fernández Esther, Ferrer Santiago, Gabarró Raquel, Gamo Francisco J, García Mercedes, Jiménez-Díaz María B, Lafuente María J, León María L, Martínez María S, Minick Douglas, Prats Sara, Puente Margarita, Rueda Lourdes, Sandoval Elena, Santos-Villarejo Angel, Witty Michael, Calderón Félix

机构信息

Tres Cantos, Medicines Development Campus, DDW, GlaxoSmithKline , Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.

Medicines for Malaria Venture (MMV) , 20 route de Pré-Bois, 1215 Geneva 15, Switzerland.

出版信息

ACS Med Chem Lett. 2014 Mar 26;5(6):657-61. doi: 10.1021/ml500015r. eCollection 2014 Jun 12.

DOI:10.1021/ml500015r
PMID:24944739
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4060931/
Abstract

Antiparasitic oral drugs have been associated to lipophilic molecules due to their intrinsic permeability. However, these kind of molecules are associated to numerous adverse effects, which have been extensively studied. Within the Tres Cantos Antimalarial Set (TCAMS) we have identified two small, soluble and simple hits that even presenting antiplasmodial activities in the range of 0.4-0.5 μM are able to show in vivo activity.

摘要

由于其固有的渗透性，抗寄生虫口服药物与亲脂性分子有关。然而，这类分子与众多不良反应相关，这些不良反应已得到广泛研究。在特雷斯坎托斯抗疟药物组合（TCAMS）中，我们鉴定出了两种小的、可溶且结构简单的活性化合物，它们即使在0.4 - 0.5 μM范围内呈现抗疟原虫活性，也能够表现出体内活性。