synthesis of [4-(2-hydroxyphenyl)thiazol-2-yl]methanones as potential bioisosteres of salicylidene acylhydrazides合成[4 -(2-hydroxyphenyl)thiazol-2-yl]methanones的潜在bioisosteres salicylidene acylhydrazides.pdfVIP

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synthesis of [4-(2-hydroxyphenyl)thiazol-2-yl]methanones as potential bioisosteres of salicylidene acylhydrazides合成[4 -(2-hydroxyphenyl)thiazol-2-yl]methanones的潜在bioisosteres salicylidene acylhydrazides.pdf

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synthesis of [4-(2-hydroxyphenyl)thiazol-2-yl]methanones as potential bioisosteres of salicylidene acylhydrazides合成[4 -(2-hydroxyphenyl)thiazol-2-yl]methanones的潜在bioisosteres salicylidene acylhydrazides

Molecules 2010, 15, 6019-6034; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis of [4-(2-Hydroxyphenyl)thiazol-2-yl]methanones as Potential Bioisosteres of Salicylidene Acylhydrazides J. Mikael Hillgren, Markus K. Dahlgren, Tam M. To and Mikael Elofsson * Department of Chemistry, Umeå University, SE-90187, Umeå, Sweden * Author to whom correspondence should be addressed; E-Mail: mikael.elofsson@chem.umu.se; Tel.: +46-90-786-9328. Received: 6 July 2010; in revised form: 26 August 2010 / Accepted: 30 August 2010 / Published: 31 August 2010 Abstract: A focused library of [4-(2-hydroxyphenyl)thiazol-2-yl]methanones was prepared in a four-step synthesis with the aim to obtain potent inhibitors of type III secretion in Gram-negative bacteria. The compounds are potential bioisosteres of salicylidene acylhydrazides that are a known class of type III secretion inhibitors. Keywords: type III secretion; Suzuki coupling; Grignard addition 1. Introduction Today it is clear that resistant bacteria constitute a threat to human health and development of new antibacterial drugs is critical to extend the successful antibiotic era. Several Gram-negative pathogens including Yersinia spp., Shigella spp., Chlamydia spp., Salmonella spp., Pseudomonas aeruginosa, and enteropathogenic and enterohaemorrhagic Escherichia coli use type III secretion (T3S) of bacterial toxins to evade the human immune system an