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Title: Design, synthesis and biological evaluation of novel anthraniloyl-amp mimics as PQS biosynthesis inhibitors against pseudomonas aeruginosa resistance
Authors: Sabir, Shekh
Subramoni, Sujatha
Das, Theerthankar
Black, David StC
Rice, Scott A.
Kumar, Naresh
Keywords: Science::Chemistry
Issue Date: 2020
Source: Sabir, S., Subramoni, S., Das, T., Black, D. S., Rice, S. A., & Kumar, N. (2020). Design, Synthesis and Biological Evaluation of Novel Anthraniloyl-AMP Mimics as PQS Biosynthesis Inhibitors Against Pseudomonas aeruginosa Resistance. Molecules, 25(13), 3103-. doi:10.3390/molecules25133103
Journal: Molecules 
Abstract: The Pseudomonas quinolone system (PQS) is one of the three major interconnected quorum sensing signaling systems in Pseudomonas aeruginosa. The virulence factors PQS and HHQ activate the transcription regulator PqsR (MvfR), which controls several activities in bacteria, including biofilm formation and upregulation of PQS biosynthesis. The enzyme anthraniloyl-CoA synthetase (PqsA) catalyzes the first and critical step in the biosynthesis of quinolones; therefore, it is an attractive target for the development of anti-virulence therapeutics against Pseudomonas resistance. Herein, we report the design and synthesis of novel triazole nucleoside-based anthraniloyl- adenosine monophosphate (AMP) mimics. These analogues had a major impact on the morphology of bacterial biofilms and caused significant reduction in bacterial aggregation and population density. However, the compounds showed only limited inhibition of PQS and did not exhibit any effect on pyocyanin production.
ISSN: 1420-3049
DOI: 10.3390/molecules25133103
Rights: © 2020 The Authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SCELSE Journal Articles

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