Potent and broad-spectrum antibacterial activity of indole-based bisamidine antibiotics: synthesis and SAR of novel analogs of MBX 1066 and MBX 1090.
Potent and broad-spectrum antibacterial activity of indole-based bisamidine antibiotics: synthesis and SAR of novel analogs of MBX 1066 and MBX 1090.
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DOI：
10.1016/j.bmc.2013.10.014
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发表时间：
2013-12-15
影响因子：
3.5
通讯作者：
Bowlin TL
中科院分区：
文献类型：
--
作者：
Williams JD;Nguyen ST;Gu S;Ding X;Butler MM;Tashjian TF;Opperman TJ;Panchal RG;Bavari S;Peet NP;Moir DT;Bowlin TL
耐药细菌在临床中的普遍存在，促使人们齐心协力寻找新型抗生素，以绕过目前的耐药模式。我们以前已经描述了一组含有由两个吲哚和一个中心连接剂组成的核心的双脒类抗生素。该系列的首批化合物MBX 1066和MBX 1090对多种革兰氏阳性和革兰氏阴性细菌具有有效的抗菌性能。我们对酰胺的功能、中心连接和吲哚3位的取代基进行了系统的探索，以确定有效抗菌活性的因素。一些新合成的化合物甚至比MBX 1066和MBX 1090具有更强的广谱活性。
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.
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影响因子：
7.3
作者：
Li, Bing;Pai, Ramdas;Cardinale, Steven C.;Butler, Michelle M.;Peet, Norton P.;Moir, Donald T.;Bavari, Sina;Bowlin, Terry L.
通讯作者：
Bowlin, Terry L.
影响因子：
3.5
作者：
Anastassiadou, M;Danoun, S;Renard, P
通讯作者：
Renard, P
影响因子：
14.2
作者：
Magiorakos, A. -P.;Srinivasan, A.;Monnet, D. L.
通讯作者：
Monnet, D. L.
影响因子：
11.8
作者：
Klevens, RM;Edwards, JR;Gaynes, R
通讯作者：
Gaynes, R
影响因子：
3.6
作者：
MCMURRY, JE;FLEMING, MP;KREPSKI, LR
通讯作者：
KREPSKI, LR