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学术机构中的药物发现早期阶段和制药公司参与推进有前途的先导化合物。

Early Stages of Drug Discovery in an Academic Institution and Involvement of Pharma for Advancing Promising Leads.

出版信息

ACS Infect Dis. 2021 Jul 9;7(7):1874-1876. doi: 10.1021/acsinfecdis.1c00091. Epub 2021 Apr 19.

DOI:10.1021/acsinfecdis.1c00091
PMID:33871981
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9323184/
Abstract

In this Viewpoint, we provide a brief description of two efforts to develop drugs to treat diseases caused by tropical parasites (Malaria, human African trypanosomiasis and Chagas disease). These efforts are largely based in a University setting but draw heavily on Pharma for a complete progression from drug hit discovery to advancement toward clinical trials. The first case is the development of protein farnesyltransferase inhibitors, and the second case is a series of benzthiazoles, the target of which is being investigated.

摘要

在本观点中,我们简要描述了两项开发药物治疗热带寄生虫病(疟疾、非洲人类锥虫病和恰加斯病)的努力。这些努力主要基于大学环境,但在药物发现到临床试验推进的整个过程中严重依赖制药公司。第一个例子是法呢基转移酶抑制剂的开发,第二个例子是一系列苯并噻唑,正在研究其目标。

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本文引用的文献

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Trop Med Infect Dis. 2020 Feb 5;5(1):23. doi: 10.3390/tropicalmed5010023.
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Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.三唑并嘧啶类和咪唑并吡啶类:锥虫病的构效关系及体内疗效
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Fexinidazole: First Global Approval.非硝唑:全球首次获批。
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1-Benzyl-3-aryl-2-thiohydantoin Derivatives as New Anti- Agents: SAR and in Vivo Efficacy.1-苄基-3-芳基-2-硫代乙内酰脲衍生物作为新型抗剂:构效关系及体内疗效
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New Class of Antitrypanosomal Agents Based on Imidazopyridines.基于咪唑并吡啶的新型抗锥虫药物
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Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.2-芳基苯并噻唑-5-胺的尿素衍生物:一类新型的人类非洲锥虫病潜在药物。
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Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.取代的 2-苯基咪唑并吡啶类:一种新型的治疗人类非洲锥虫病的药物先导化合物。
J Med Chem. 2014 Feb 13;57(3):828-35. doi: 10.1021/jm401178t. Epub 2014 Jan 15.
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SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis.SCYX-7158,一种用于治疗 2 期人体非洲锥虫病的口服苯并硼烷。
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How were new medicines discovered?新药是如何发现的?
Nat Rev Drug Discov. 2011 Jun 24;10(7):507-19. doi: 10.1038/nrd3480.
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Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.结构简单、高效、对疟原虫有选择性的法尼基转移酶抑制剂,可阻止疟原虫的生长。
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