Design, synthesis and biological evaluation of novel Pseudomonas aeruginosa DNA gyrase B inhibitors

Out of 40 benzimdazoles, 12 exhibited potent QSI activity against P. aeruginosa6p, most active QSI is docked to LasR and is less toxic against HEK 293 cell line.

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Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.8b01750 ◽

2019 ◽

Vol 62 (6) ◽

pp. 2950-2973 ◽

Cited By ~ 8

Author(s):

Chenghui Shi ◽

Yinyong Zhang ◽

Ting Wang ◽

Wenchao Lu ◽

Shuhua Zhang ◽

...

Keyword(s):

Dna Gyrase ◽

Multidrug Resistant ◽

Biological Evaluation ◽

Gram Positive ◽

Design Synthesis ◽

Gram Positive Bacteria ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2016.10.038 ◽

2017 ◽

Vol 25 (1) ◽

pp. 338-349 ◽

Cited By ~ 22

Author(s):

Tihomir Tomašič ◽

Matic Mirt ◽

Michaela Barančoková ◽

Janez Ilaš ◽

Nace Zidar ◽

...

Keyword(s):

Dna Gyrase ◽

Biological Evaluation ◽

Design Synthesis ◽

Synthesis And Biological Evaluation ◽

Gyrase Inhibitors

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Design, synthesis and biological evaluation of 2-substituted 3-hydroxy-6-methyl-4H-pyran-4-one derivatives as Pseudomonas aeruginosa biofilm inhibitors

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2018.09.041 ◽

2018 ◽

Vol 158 ◽

pp. 753-766 ◽

Cited By ~ 9

Author(s):

Yi-Bin Li ◽

Jun Liu ◽

Zhi-Xing Huang ◽

Jia-Hui Yu ◽

Xiao-Fang Xu ◽

...

Keyword(s):

Pseudomonas Aeruginosa ◽

Biological Evaluation ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Design, Synthesis and Biological Evaluation of Novel Anthraniloyl-AMP Mimics as PQS Biosynthesis Inhibitors Against Pseudomonas aeruginosa Resistance

Molecules ◽

10.3390/molecules25133103 ◽

2020 ◽

Vol 25 (13) ◽

pp. 3103

Author(s):

Shekh Sabir ◽

Sujatha Subramoni ◽

Theerthankar Das ◽

David StC. Black ◽

Scott A. Rice ◽

...

Keyword(s):

Pseudomonas Aeruginosa ◽

Biofilm Formation ◽

Adenosine Monophosphate ◽

Biological Evaluation ◽

Bacterial Biofilms ◽

Design Synthesis ◽

Signaling Systems ◽

Design And Synthesis ◽

Bacterial Aggregation ◽

Synthesis And Biological Evaluation

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.

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