The Goossen decarboxylative coupling reaction enables the union of thiazole-2-carboxylic acids with a 2-pyridyl triflate, leading to the formation of pyridine-thiazole clusters of the kind found in thiopeptide antibiotics. The method avoids problematic or technically challenging reaction sequences involving 2-thiazolyl organometallics, facilitating the investigation of the structure-activity relationship of the thiopeptides.
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http://dx.doi.org/10.1021/acs.joc.4c02362 | DOI Listing |
ACS Infect Dis
December 2024
Faculty of Medicine and Health, University of Sydney, Sydney, NSW 2015, Australia.
Persiathiacin A is a novel thiopeptide antibiotic produced by species UTMC 2448. It has potent activity against methicillin-resistant (MRSA) and . Thiopeptides, including persiathiacin A, exhibit antibacterial activity by inhibiting protein synthesis.
View Article and Find Full Text PDFJ Org Chem
December 2024
Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, BC V6T 1Z1, Canada.
The Goossen decarboxylative coupling reaction enables the union of thiazole-2-carboxylic acids with a 2-pyridyl triflate, leading to the formation of pyridine-thiazole clusters of the kind found in thiopeptide antibiotics. The method avoids problematic or technically challenging reaction sequences involving 2-thiazolyl organometallics, facilitating the investigation of the structure-activity relationship of the thiopeptides.
View Article and Find Full Text PDFJ Nanobiotechnology
October 2024
Innovative Team of Antimicrobial Peptides and Alternatives to Antibiotics, Gene Engineering Laboratory, Feed Research Institute, Chinese Academy of Agricultural Sciences, 12 Zhongguancun Nandajie St., Haidian District, Beijing, 100081, China.
Antibiotics (Basel)
September 2024
Gene Engineering Laboratory, Feed Research Institute, Chinese Academy of Agricultural Sciences, Beijing 100081, China.
Wound infections caused by often result in localized suppurative lesions that severely impede the healing process, so it is urgent to develop a dress with efficient antimicrobial and pro-healing functions. In this study, the bifunctional injectable hydrogel lactoferrin (Lf)/NZ2114/lithium magnesium silicate hydrogel (LMSH) was first successfully prepared through the electrostatic interaction method. The physical, biological, and efficacy properties are systematically analyzed with good shear-thinning capacity and biocompatibility.
View Article and Find Full Text PDFACS Infect Dis
September 2024
Department of Chemistry, University of Warwick, Coventry CV4 7AL, U.K.
Thiopeptides are ribosomally biosynthesized and post-translationally modified peptides (RiPPs) that potently inhibit the growth of Gram-positive bacteria by targeting multiple steps in protein biosynthesis. The poor pharmacological properties of thiopeptides, particularly their low aqueous solubility, has hindered their development into clinically useful antibiotics. Antimicrobial activity screens of a library of Actinomycetota extracts led to discovery of the novel polyglycosylated thiopeptides persiathiacins A and B from sp.
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