Drug resistance reversal potential of multifunctional thieno[3,2-c]pyran via potentiation of antibiotics in MDR P. aeruginosa

descriptionPublicationkeyboard_double_arrow_right Article 01 Oct 2021 English Publisher:Elsevier BVJournal:Biomedicine & Pharmacotherapy, volume 142, page 112,084 (issn: 0753-3322,

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Authors: Gaurav Raj, Dwivedi; Reeta, Rai; Ramendra, Pratap; Khusbu, Singh; Sanghamitra, Pati; Satya Narayan, Sahu; Rajni, Kant; +2 Authors

doi: 10.1016/j.biopha.2021.112084

pmid: 34449308

Drug resistance reversal potential of multifunctional thieno[3,2-c]pyran via potentiation of antibiotics in MDR P. aeruginosa

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Abstract

We explored the antibacterial potential (alone and combination) against multidrug resistant (MDR) Pseudomonas aeruginosa isolates KG-P2 using synthesized thieno[3,2-c]pyran-2-ones in combination with different antibiotics. Out of 14 compounds, two compounds (3g and 3l) abridged the MIC of tetracycline (TET) by 16 folds. Compounds was killing the KG-P2 cells, in time dependent manner, lengthened post-antibiotic effect (PAE) of TET and found decreased the mutant prevention concentration (MPC) of TET. In ethidium bromide efflux experiment, two compounds repressed the drug transporter (efflux pumps) which is further supported by molecular docking of these compounds with efflux complex MexAB-OprM. In another study, these compounds inhibited the synthesis of biofilm.

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Keywords

Time Factors, Drug Synergism, Microbial Sensitivity Tests, Tetracycline, Anti-Bacterial Agents, Molecular Docking Simulation, Structure-Activity Relationship, Pyrones, Biofilms, Drug Resistance, Multiple, Bacterial, Pseudomonas aeruginosa, Drug Therapy, Combination

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