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

Authors :: Dwivedi GR
Rai R
Pratap R
Singh K
Pati S
Sahu SN
Kant R
Darokar MP
Yadav DK
Source :: Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie [Biomed Pharmacother] 2021 Oct; Vol. 142, pp. 112084. Date of Electronic Publication: 2021 Aug 24.
Publication Year :: 2021
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.<br /> (Copyright © 2021 The Authors. Published by Elsevier Masson SAS.. All rights reserved.)

Subjects :: Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Biofilms drug effects
Drug Resistance, Multiple, Bacterial
Drug Synergism
Drug Therapy, Combination
Microbial Sensitivity Tests
Molecular Docking Simulation
Pyrones chemical synthesis
Pyrones chemistry
Structure-Activity Relationship
Tetracycline pharmacology
Time Factors
Anti-Bacterial Agents pharmacology
Pseudomonas aeruginosa drug effects
Pyrones pharmacology

Full Text Access

Tools