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2
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本文引用的文献

1
10 x '20 Progress--development of new drugs active against gram-negative bacilli: an update from the Infectious Diseases Society of America.10 x '20 进展——开发针对革兰氏阴性杆菌的新型药物：来自美国传染病学会的最新进展。
Clin Infect Dis. 2013 Jun;56(12):1685-94. doi: 10.1093/cid/cit152. Epub 2013 Apr 17.
2
The role of the natural environment in the emergence of antibiotic resistance in gram-negative bacteria.自然环境在革兰氏阴性菌抗生素耐药性出现中的作用。
Lancet Infect Dis. 2013 Feb;13(2):155-65. doi: 10.1016/S1473-3099(12)70317-1.
3
A C-H borylation approach to Suzuki-Miyaura coupling of typically unstable 2-heteroaryl and polyfluorophenyl boronates.一种 C-H 硼化方法，用于通常不稳定的 2-杂芳基和多氟代苯基硼酸酯的铃木-宫浦偶联反应。
Org Lett. 2012 Aug 17;14(16):4266-9. doi: 10.1021/ol301570t. Epub 2012 Aug 2.
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New classes of antibiotics.新型抗生素。
Curr Opin Pharmacol. 2012 Oct;12(5):535-44. doi: 10.1016/j.coph.2012.07.004. Epub 2012 Jul 26.
5
Multidrug-resistant, extensively drug-resistant and pandrug-resistant bacteria: an international expert proposal for interim standard definitions for acquired resistance.耐多药、广泛耐药和全耐药细菌：获得性耐药的国际专家临时标准定义建议
Clin Microbiol Infect. 2012 Mar;18(3):268-81. doi: 10.1111/j.1469-0691.2011.03570.x. Epub 2011 Jul 27.
6
Novel classes of antibiotics or more of the same?新型抗生素还是更多的同类抗生素？
Br J Pharmacol. 2011 May;163(1):184-94. doi: 10.1111/j.1476-5381.2011.01250.x.
7
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.新型双吲哚类抗菌药物对革兰氏阳性和革兰氏阴性临床分离株的体外活性比较。
Antimicrob Agents Chemother. 2010 Sep;54(9):3974-7. doi: 10.1128/AAC.00484-10. Epub 2010 Jul 12.
8
Synthesis and biological evaluation of botulinum neurotoxin a protease inhibitors.肉毒神经毒素 A 蛋白酶抑制剂的合成与生物学评价。
J Med Chem. 2010 Mar 11;53(5):2264-76. doi: 10.1021/jm901852f.
9
Infections by pandrug-resistant gram-negative bacteria: clinical profile, therapeutic management, and outcome in a series of 21 patients.泛耐药革兰氏阴性菌感染：21 例患者的临床特征、治疗管理和转归。
Eur J Clin Microbiol Infect Dis. 2010 Mar;29(3):301-5. doi: 10.1007/s10096-009-0857-7.
10
Novel broad-spectrum bis-(imidazolinylindole) derivatives with potent antibacterial activities against antibiotic-resistant strains.对耐药菌株具有强效抗菌活性的新型广谱双（咪唑啉吲哚）衍生物。
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基于吲哚的双脒类抗生素具有强大而广谱的抗菌活性：MBX 1066 和 MBX 1090 新型类似物的合成及 SAR 研究。

Potent and broad-spectrum antibacterial activity of indole-based bisamidine antibiotics: synthesis and SAR of novel analogs of MBX 1066 and MBX 1090.

机构信息

Microbiotix, Inc., 1 Innovation Drive, Worcester, MA 01604, USA.

出版信息

Bioorg Med Chem. 2013 Dec 15;21(24):7790-806. doi: 10.1016/j.bmc.2013.10.014. Epub 2013 Oct 25.

DOI:10.1016/j.bmc.2013.10.014
PMID:24239389
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3906850/
Abstract

The prevalence of drug-resistant bacteria in the clinic has propelled a concerted effort to find new classes of antibiotics that will circumvent current modes of resistance. We have previously described a set of bisamidine antibiotics that contains a core composed of two indoles and a central linker. The first compounds of the series, MBX 1066 and MBX 1090, have potent antibacterial properties against a wide range of Gram-positive and Gram-negative bacteria. We have conducted a systematic exploration of the amidine functionalities, the central linker, and substituents at the indole 3-position to determine the factors involved in potent antibacterial activity. Some of the newly synthesized compounds have even more potent and broad-spectrum activity than MBX 1066 and MBX 1090.

摘要

临床上耐药菌的流行促使人们齐心协力寻找新的抗生素类别，以规避当前的耐药模式。我们之前描述了一组双脒类抗生素，其核心由两个吲哚和一个中央连接子组成。该系列的第一批化合物 MBX 1066 和 MBX 1090 对多种革兰氏阳性和革兰氏阴性菌具有很强的抗菌活性。我们对脒基官能团、中央连接子以及吲哚 3 位的取代基进行了系统的研究，以确定与强抗菌活性相关的因素。一些新合成的化合物比 MBX 1066 和 MBX 1090 具有更强和更广谱的活性。