- Title
- Synthesis and MRSA PK inhibitory activity of thiazole containing deoxytopsentin analogues
- Creator
- Veale, Clinton G L, Lobb, Kevin A, Zoraghi, Roya, Morrison, James P, Reiner, Neil E, Andersen, Raymond J, Davies-Coleman, Michael T
- Subject
- To be catalogued
- Date
- 2014
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/448028
- Identifier
- vital:74692
- Identifier
- xlink:href="https://doi.org/10.1016/j.tet.2014.09.007"
- Description
- The public health care crisis caused by the emergence of drug resistant bacterial strains, e.g., methicillin resistant Staphylococcus aureus (MRSA) has underlined the urgent need to accelerate the discovery of new chemical entities active against antibiotic resistant bacteria. We report here the synthesis of a series thiazole containing deoxytopsentin analogues, which show moderate activity against a target MRSA pyruvate kinase enzyme: an evolutionary conserved hub protein critical for bacterial survival. A Hantzsch thiazole coupling between a-oxo-1H-indole-3-thioacetamides and 2-bromo-1-(1H-indol-3-yl)-ethanones provided facile access to the thiazole containing deoxytopsentin compounds.
- Format
- computer, online resource, application/pdf, 1 online resource (9 pages), pdf
- Publisher
- Elsevier
- Language
- English
- Relation
- Tetrahedron, Veale, C.G., Lobb, K.A., Zoraghi, R., Morrison, J.P., Reiner, N.E., Andersen, R.J. and Davies-Coleman, M.T., 2014. Synthesis and MRSA PK inhibitory activity of thiazole containing deoxytopsentin analogues. Tetrahedron, 70(43), pp.7845-7853, Tetrahedron volume 70 number 43 p. 7845 2014 1464-5416
- Rights
- Publisher
- Rights
- Use of this resource is governed by the terms and conditions of the Elsevier Terms and Conditions Statement (https://www.elsevier.com/legal/elsevier-website-terms-and-conditions)
- Rights
- Closed Access
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Collections
Veale, Clinton G L (Dr)
Lobb, Kevin Allan (Assoc Prof)
RU Department of Chemistry
SDG 03. Good Health and Well-Being
| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details Download | SOURCE1 | Synthesis and MRSA PK inhibitory activity of thiazole containing deoxytopsentin analogues.pdf | 791 KB | Adobe Acrobat PDF | View Details Download |