Synthesis and Antimicrobial Activity of Phosphonopeptide Derivatives Incorporating Single and Dual Inhibitors

Molecules

JohnD. Perry¹  EmmaC.L. Marrs¹  Sylvain Orenga²  KengTiong Ng³  Mark Gray³  RosaleenJ. Anderson³ 

[1] Microbiology Department, Freeman Hospital, High Heaton, Newcastle upon Tyne NE7 7DN, UK;R&D Microbiologie, bioMérieux, 3 Route de Port Michaud, 38390 La Balme-les-Grottes, France;Sunderland Pharmacy School, University of Sunderland, Sunderland SR1 3SD, UK;

关键词: bacterial detection;    suicide substrates;    fosfalin;    β-chloroalanine;   

DOI  :  10.3390/molecules25071557

来源: DOAJ

【 摘 要 】

In diagnostic microbiology, culture media are widely used for detection of pathogenic bacteria. Such media employ various ingredients to optimize detection of specific pathogens such as chromogenic enzyme substrates and selective inhibitors to reduce the presence of commensal bacteria. Despite this, it is rarely possible to inhibit the growth of all commensal bacteria, and thus pathogens can be overgrown and remain undetected. One approach to attempt to remedy this is the use of “suicide substrates” that can target specific bacterial enzymes and selectively inhibit unwanted bacterial species. With the purpose of identifying novel selective inhibitors, six novel phosphonopeptide derivatives based on d/l-fosfalin and β-chloro-l-alanine were synthesized and tested on 19 different strains of clinically relevant bacteria. Several compounds show potential as useful selective agents that could be exploited in the recovery of several bacterial pathogens including Salmonella, Pseudomonas aeruginosa, and Listeria.

【 授权许可】

Unknown