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新型抗结核多药耐药化合物的药物发现进展

Advances in Drug Discovery of New Antitubercular Multidrug-Resistant Compounds.

作者信息

Fernandes Guilherme Felipe Dos Santos, Man Chin Chung, Dos Santos Jean Leandro

机构信息

Institute of Chemistry, São Paulo State University (UNESP), Araraquara 14800060, Brazil.

School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara 14800903, Brazil.

出版信息

Pharmaceuticals (Basel). 2017 Jun 1;10(2):51. doi: 10.3390/ph10020051.

DOI:10.3390/ph10020051
PMID:28587160
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5490408/
Abstract

Tuberculosis (TB), a disease caused mainly by the , is according to the World Health Organization (WHO) the infectious disease responsible for the highest number of deaths worldwide. The increased number of multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains, and the ineffectiveness of the current treatment against latent tuberculosis are challenges to be overcome in the coming years. The scenario of drug discovery becomes alarming when it is considered that the number of new drugs does not increase proportionally to the emergence of drug resistance. In this review, we will demonstrate the current advances in antitubercular drug discovery, focusing on the research of compounds with potent antituberculosis activity against MDR-TB strains. Herein, active compounds against MDR-TB with minimum inhibitory concentrations (MICs) less than 11 µM and low toxicity published in the last 4 years in the databases PubMed, Web of Science and Scopus will be presented and discussed.

摘要

结核病（TB）主要由[此处原文缺失相关内容]引起，据世界卫生组织（WHO）称，它是全球导致死亡人数最多的传染病。耐多药（MDR-TB）和广泛耐药（XDR-TB）菌株数量的增加，以及当前针对潜伏性结核病治疗的无效性，是未来几年需要克服的挑战。当考虑到新药数量并未与耐药性的出现成比例增加时，药物研发的情况就变得令人担忧。在本综述中，我们将展示抗结核药物研发的当前进展，重点关注对耐多药结核菌株具有强效抗结核活性的化合物的研究。在此，将展示并讨论过去4年在PubMed、Web of Science和Scopus数据库中发表的对耐多药结核杆菌最低抑菌浓度（MIC）小于11µM且毒性低的活性化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/9c28e1af838a/pharmaceuticals-10-00051-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/d3a0b293d78a/pharmaceuticals-10-00051-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/c92f6ae7eb39/pharmaceuticals-10-00051-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/6d0c4b5353c5/pharmaceuticals-10-00051-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/4b2f57d167d7/pharmaceuticals-10-00051-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/02cfd1fe3ce0/pharmaceuticals-10-00051-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/b6775aa5a8cd/pharmaceuticals-10-00051-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/b186a40b01f0/pharmaceuticals-10-00051-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/9627be81e7c4/pharmaceuticals-10-00051-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/561b4c884f2b/pharmaceuticals-10-00051-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/9c28e1af838a/pharmaceuticals-10-00051-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/d3a0b293d78a/pharmaceuticals-10-00051-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/e3aeb90bae02/pharmaceuticals-10-00051-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/aa497e1684d7/pharmaceuticals-10-00051-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/e3484426f99a/pharmaceuticals-10-00051-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/820708648460/pharmaceuticals-10-00051-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/c92f6ae7eb39/pharmaceuticals-10-00051-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/6d0c4b5353c5/pharmaceuticals-10-00051-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/4b2f57d167d7/pharmaceuticals-10-00051-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/02cfd1fe3ce0/pharmaceuticals-10-00051-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/b6775aa5a8cd/pharmaceuticals-10-00051-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/b186a40b01f0/pharmaceuticals-10-00051-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/9627be81e7c4/pharmaceuticals-10-00051-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/561b4c884f2b/pharmaceuticals-10-00051-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba25/5490408/9c28e1af838a/pharmaceuticals-10-00051-g014.jpg

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