- Title
- MRSA pyruvate kinase inhibitory activity of synthetically derived thiazole containing deoxytopsentin analogues
- Creator
- Veale, Clinton G L, Zoraghi, Roya, Lobb, Kevin A, 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/10962/448923
- Identifier
- vital:74771
- Identifier
- xlink:href="https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0034-1382365"
- Description
- The health care crisis caused by methicillin resistant Staphylococcus aureus (MRSA) is due in part to a lack of fundamental drug discovery research into new antibiotics with novel modes of action. Marine bis-indole alkaloids have proved to be effective in vitro antibacterials. We present the synthesis of thiazole containing analogues of the marine natural product MRSA pyruvate kinase (PK) inhibitor, 6-bromodeoxytopsenin. The synthetic analogues showed moderate activity compared to the marine natural product against MRSA PK, an evolutionary conserved hub protein critical for bacterial survival. Our synthesis, via a Hantzsch thiazole condensation of α-oxo-1H-indole-3-thioacetamides with 2-bromo-1-(1H-indol-3-yl)-ethanones provided several challenges.
- Format
- computer, online resource, application/pdf, 1 online resource (1 pages), pdf
- Publisher
- Thieme
- Language
- English
- Relation
- Planta Medica, Veale, C.G.L., Zoraghi, R., Lobb, K.A., Reiner, N.E., Andersen, R.J. and Davies-Coleman, M.T., 2014. MRSA pyruvate kinase inhibitory activity of synthetically derived thiazole containing deoxytopsentin analogues. Planta Medica, 80(10), p.CL32, Planta Medica volume 80 number 10 p. CL32 2014 1439-0221
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- Publisher
- Rights
- Use of this resource is governed by the terms and conditions of the Thieme Privacy Statement (https://www.thieme.de/de/thieme-gruppe/privacy-policy-statement-Thieme-EN.htm)
- 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 | SOURCE1 | MRSA pyruvate kinase inhibitory activity of synthetically derived thiazole containing deoxytopsentin analogues.pdf | 652 KB | Adobe Acrobat PDF | View Details |