期刊
ANTIBIOTICS-BASEL
卷 9, 期 7, 页码 -出版社
MDPI
DOI: 10.3390/antibiotics9070369
关键词
1; 2; 3-dithiazole; 1; 2; 3-thiaselenazole; sulfur extrusion; selenium dioxide; antimicrobial; antibacterial; antifungal
资金
- Wellcome Trust (UK)
- University of Queensland (Australia)
- Ministry of Education and Science of the Russian Federation [FENU-2020-0019 (2020073GZ)]
- Biocenter Finland/DDCB
We report our investigations into the underlying differences between 1,2,3-dithiazole and their ultra-rare counterpart, 1,2,3-thiaselenazole. This rare 1,2,3-thiaselenazole chemotype was afforded by sulfur extrusion and selenium insertion into the preconstructed 1,2,3-dithiazoles. We built a library of matched paired compounds to compare and contrast the two ring systems. This led to the development of both narrow and broad-spectrum antimicrobial compounds with sub-micro molar potency, limited to no toxicity and a further understanding of the transition state electronics through molecular simulations. We also identified the potent 4,5,6-trichlorocyclopenta[d][1,2,3]thiaselenazole11a, for use againstCandida albicans,Cryptococcus neoformans var. grubii,Staphylococcus aureusandAcinetobacter baumannii, all of which have limited clinical treatment options. The 1,2,3-thiaselenazole represents a new class of potential compounds for the treatment of a host of multi-resistant hospital derived infections.
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