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本文引用的文献

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Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry.一系列适用于从活性分子到先导化合物化学转化的新型抗疟药的鉴定及体外ADME评估
ACS Med Chem Lett. 2012 May 28;3(7):570-3. doi: 10.1021/ml300091c. eCollection 2012 Jul 12.
2
Deciphering the Resistance-Counteracting Functions of Ferroquine in Plasmodium falciparum-Infected Erythrocytes.解析磷酸氯喹对恶性疟原虫感染红细胞的抗耐药作用
ACS Med Chem Lett. 2012 Apr 13;3(6):480-3. doi: 10.1021/ml300062q. eCollection 2012 Jun 14.
3
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.
4
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.恶性疟原虫二氢乳清酸脱氢酶强效抑制剂用于疟疾治疗的优化
ACS Med Chem Lett. 2011 Jul 11;2(9):708-13. doi: 10.1021/ml200143c. eCollection 2011 Sep 8.
5
Extracting SAR Information from a Large Collection of Anti-Malarial Screening Hits by NSG-SPT Analysis.通过NSG-SPT分析从大量抗疟筛选命中物中提取SAR信息。
ACS Med Chem Lett. 2011 Jan 5;2(3):201-6. doi: 10.1021/ml100240z. eCollection 2011 Mar 10.
6
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.
7
Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria.新型苯并[a]吩噁嗪SSJ-183作为疟疾候选药物的发现。
ACS Med Chem Lett. 2010 Jul 12;1(7):360-4. doi: 10.1021/ml100120a. eCollection 2010 Oct 14.
8
G6PD deficiency: global distribution, genetic variants and primaquine therapy.葡萄糖-6-磷酸脱氢酶(G6PD)缺乏症:全球分布、遗传变异和伯氨喹治疗。
Adv Parasitol. 2013;81:133-201. doi: 10.1016/B978-0-12-407826-0.00004-7.
9
New bis-thiazolium analogues as potential antimalarial agents: design, synthesis, and biological evaluation.新型双噻唑啉类似物作为潜在的抗疟药物:设计、合成与生物评价。
J Med Chem. 2013 Jan 24;56(2):496-509. doi: 10.1021/jm3014585. Epub 2013 Jan 4.
10
Targeting the ERAD pathway via inhibition of signal peptide peptidase for antiparasitic therapeutic design.通过抑制信号肽肽酶靶向 ERAD 途径用于抗寄生虫治疗设计。
Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21486-91. doi: 10.1073/pnas.1216016110. Epub 2012 Dec 11.

疟疾药物发现的最新进展。

Recent advances in malaria drug discovery.

机构信息

Drug Discovery for Tropical Diseases, Suite 230, San Diego, CA 92121, USA.

出版信息

Bioorg Med Chem Lett. 2013 May 15;23(10):2829-43. doi: 10.1016/j.bmcl.2013.03.067. Epub 2013 Mar 27.

DOI:10.1016/j.bmcl.2013.03.067
PMID:23587422
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3762334/
Abstract

This digest covers some of the most relevant progress in malaria drug discovery published between 2010 and 2012. There is an urgent need to develop new antimalarial drugs. Such drugs can target the blood stage of the disease to alleviate the symptoms, the liver stage to prevent relapses, and the transmission stage to protect other humans. The pipeline for the blood stage is becoming robust, but this should not be a source of complacency, as the current therapies set a high standard. Drug discovery efforts directed towards the liver and transmission stages are in their infancy but are receiving increasing attention as targeting these stages could be instrumental in eradicating malaria.

摘要

本文摘涵盖了 2010 年至 2012 年间发表的疟疾药物发现领域最相关的进展。开发新的抗疟药物迫在眉睫。这些药物可以针对疾病的血液阶段以缓解症状,针对肝脏阶段以预防复发,针对传播阶段以保护其他人。血液阶段的研发管道正在变得强大,但这不应成为自满的理由,因为目前的疗法设定了高标准。针对肝脏和传播阶段的药物发现工作尚处于起步阶段,但越来越受到关注,因为针对这些阶段可能是消除疟疾的关键。