scholarly journals Design, synthesis and biological evaluation of 1,2,3-triazole based 2-aminobenzimidazoles as novel inhibitors of LasR dependent quorum sensing in Pseudomonas aeruginosa

RSC Advances ◽  
2019 ◽  
Vol 9 (50) ◽  
pp. 29273-29292 ◽  
Author(s):  
Singireddi Srinivasarao ◽  
Adinarayana Nandikolla ◽  
Shashidhar Nizalapur ◽  
Tsz Tin Yu ◽  
Sravani Pulya ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Quorum Sensing ◽  
Cell Line ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Hek 293 ◽  
Line P ◽  
Synthesis And Biological Evaluation ◽  
Hek 293 Cell Line

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.

Design, Synthesis and Biological Evaluation of Triazole-Containing 2-Phenylindole and Salicylic Acid as Quorum Sensing Inhibitors Against Pseudomonas aeruginosa

2018 ◽  
Vol 3 (32) ◽  
pp. 9170-9180 ◽  
Author(s):  
Singireddi Srinivasarao ◽  
Shashidhar Nizalapur ◽  
Tsz Tin Yu ◽  
Daniel Stanley Wenholz ◽  
Prakruti Trivedi ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Salicylic Acid ◽  
Quorum Sensing ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Quorum Sensing Inhibitors ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of non-natural modulators of quorum sensing in Pseudomonas aeruginosa

2012 ◽  
Vol 10 (30) ◽  
pp. 6032 ◽  
Author(s):  
James T. Hodgkinson ◽  
Warren R. J. D. Galloway ◽  
Megan Wright ◽  
Ioulia K. Mati ◽  
Rebecca L. Nicholson ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Quorum Sensing ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of novel unsymmetrical azines as quorum sensing inhibitors

RSC Advances ◽  
2015 ◽  
Vol 5 (97) ◽  
pp. 80027-80038 ◽  
Author(s):  
Sumit S. Chourasiya ◽  
Deepika Kathuria ◽  
Shaminder Singh ◽  
Vijay C. Sonawane ◽  
Asit K. Chakraborti ◽  
...  
Keyword(s):  
Quorum Sensing ◽  
Biological Evaluation ◽  
One Pot ◽  
Design Synthesis ◽  
Quorum Sensing Inhibitors ◽  
Synthesis And Biological Evaluation

In this report, novel unsymmetrical azines have been designed and synthesised by using one pot approach. Further, they were evaluated as quorum sensing inhibitors.

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

Molecules ◽  
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.

scholarly journals Design, synthesis, and biological evaluation of symmetrical azine derivatives as novel tyrosinase inhibitors

BMC Chemistry ◽  
2021 ◽  
Vol 15 (1) ◽  
Author(s):  
Somaye Karimian ◽  
Fatemeh Kazemi ◽  
Mahshid Attarroshan ◽  
Maryam Gholampour ◽  
Shiva Hemmati ◽  
...  
Keyword(s):  
Cell Line ◽  
Inhibitory Activity ◽  
Binding Mode ◽  
Positive Control ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Substrate Complex ◽  
Enzyme Substrate ◽  
Melanoma B16f10 ◽  
Synthesis And Biological Evaluation

AbstractA series of symmetrical azine derivatives containing different substituted benzyl moieties were designed, synthesized, and evaluated for their inhibitory activity against tyrosinase. The results showed that compounds 3e, 3f, 3h, 3i, 3j, and 3k possess effective tyrosinase inhibition with IC50 values ranging from 7.30 μM to 62.60 μM. Particularly, compounds 3f displayed around three-fold improvement in the potency (IC50 = 7.30 ± 1.15 μM) compared to that of kojic acid (IC50 = 20.24 ± 2.28 μM) as the positive control. Kinetic study of compound 3f confirmed uncompetitive inhibitory activity towards tyrosinase indicating that it can bind to enzyme–substrate complex. Next, molecular docking analysis was performed to study the interactions and binding mode of the most potent compound 3f in the tyrosinase active site. Besides, the cytotoxicity of 3f, as well as its potency to reduce the melanin content were also measured on invasive melanoma B16F10 cell line. Also, 3f exhibited above 82% cell viability in the A375 cell line at 10 µM. Consequently, compounds 3f could be introduced as a potent tyrosinase inhibitor that might be a promising candidate in the cosmetics, medicine, and food industry.

Sign in / Sign up

Export Citation Format

Share Document