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Simplified novel muraymycin analogues ; using a serine template strategy for linking key pharmacophores
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Patel, Bhautikkumar, Kerr, Rachel, Malde, Alpeshkumar K., Zunk, Matthew, Bugg, Timothy D. H., Grant, Gary and Rudrawar, Santosh (2020) Simplified novel muraymycin analogues ; using a serine template strategy for linking key pharmacophores. ChemMedChem, 15 (15). pp. 1429-1438. doi:10.1002/cmdc.202000033 ISSN 1860-7179.
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WRAP-Simplified-novel-muraymycin-analogues-pharmacophores-Bugg-2020.pdf - Accepted Version - Requires a PDF viewer. Download (1090Kb) | Preview |
Official URL: https://doi.org/10.1002/cmdc.202000033
Abstract
The present status of antibiotic research requires the urgent invention of novel agents that act on multidrug-resistant bacteria. The World Health Organization has classified antibiotic-resistant bacteria into critical, high and medium priority according to the urgency of need for new antibiotics. Naturally occurring uridine-derived "nucleoside antibiotics" have shown promising activity against numerous priority resistant organisms by inhibiting the transmembrane protein MraY (translocase I), which is yet to be explored in a clinical context. The catalytic activity of MraY is an essential process for bacterial cell viability and growth including that of priority organisms. Muraymycins are one subclass of naturally occurring MraY inhibitors. Despite having potent antibiotic properties, the structural complexity of muraymycins advocates for simplified analogues as potential lead structures. Herein, we report a systematic structure-activity relationship (SAR) study of serine template-linked, simplified muraymycin-type analogues. This preliminary SAR lead study of serine template analogues successfully revealed that the complex structure of naturally occurring muraymycins could be easily simplified to afford bioactive scaffolds against resistant priority organisms. This study will pave the way for the development of novel antibacterial lead compounds based on a simplified serine template. [Abstract copyright: © 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.]
| Item Type: | Journal Article | |||||||||||||||
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| Subjects: | Q Science > QD Chemistry Q Science > QP Physiology R Medicine > RM Therapeutics. Pharmacology R Medicine > RS Pharmacy and materia medica |
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| Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry | |||||||||||||||
| SWORD Depositor: | Library Publications Router | |||||||||||||||
| Library of Congress Subject Headings (LCSH): | Antibiotics, Anti-infective agents, Natural products, Nucleosides, Pharmaceutical chemistry, Drug resistance in microorganisms | |||||||||||||||
| Journal or Publication Title: | ChemMedChem | |||||||||||||||
| Publisher: | Wiley - V C H Verlag GmbH & Co. KGaA | |||||||||||||||
| ISSN: | 1860-7179 | |||||||||||||||
| Official Date: | 5 August 2020 | |||||||||||||||
| Dates: |
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| Volume: | 15 | |||||||||||||||
| Number: | 15 | |||||||||||||||
| Page Range: | pp. 1429-1438 | |||||||||||||||
| DOI: | 10.1002/cmdc.202000033 | |||||||||||||||
| Status: | Peer Reviewed | |||||||||||||||
| Publication Status: | Published | |||||||||||||||
| Reuse Statement (publisher, data, author rights): | "This is the peer reviewed version of the following article: Patel, B., Kerr, R.V., Malde, A.K., Zunk, M., Bugg, T.D.H., Grant, G. and Rudrawar, S. (2020), Simplified Novel Muraymycin Analogues; using a Serine Template Strategy for Linking Key Pharmacophores. ChemMedChem. doi:10.1002/cmdc.202000033, which has been published in final form at https://doi.org/10.1002/cmdc.202000033. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions." | |||||||||||||||
| Access rights to Published version: | Restricted or Subscription Access | |||||||||||||||
| Date of first compliant deposit: | 18 June 2020 | |||||||||||||||
| Date of first compliant Open Access: | 31 May 2021 | |||||||||||||||
| RIOXX Funder/Project Grant: |
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