Tetrahydropyridine derivative as efflux inhibitor in Mycobacterium abscessus

Authors: Vianna JS, Ramis IB, Bierhals D, von Groll A, Ramos DF, Zanatta N, Lourenço MC, Viveiros M, Almeida da Silva PE
Publication Year: 2019
Journal: Journal of General Virology
Link: https://www.ncbi.nlm.nih.gov/pubmed/30630106

OBJECTIVES: This study aimed to evaluate a tetrahydropyridine derivative (THP) as a potential inhibitor of the efflux mechanism and modulator of the high level of antimicrobial resistance usually observed in members of the Mycobacterium abscessus (M. abscessus) group. METHODS: The strain M. abscessus subsp. abscessus (ATCC 19997) was used as reference, in addition to three […]
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In silico and in vitro evaluation of tetrahydropyridine compounds as efflux inhibitors in Mycobacterium abscessus

Authors: Ramis IB, Vianna JS, Silva Junior L, von Groll A, Ramos DF, Zanatta N, Viveiros M, Silva PEAD
Publication Year: 2019
Journal: Tuberculosis
Link: https://www.sciencedirect.com/science/article/pii/S1472979219300654

Herein, we evaluated tetrahydropyridine (THP) compounds (NUNM) as antimicrobials and inhibitors of the efflux mechanism in M. abscessus. subsp. abscessus. The modulation factor (MF) of efflux inhibitors was calculated from the minimum inhibitory concentrations (MICs) of amikacin (AMI), ciprofloxacin (CIP) and clarithromycin (CLA) in the absence and presence of subinhibitory concentrations of the NUNM compounds and canonical […]
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In vitro and in silico analysis of the efficiency of tetrahydropyridines as drug efflux inhibitors in Escherichia coli

Authors: Almeida da Silva PE, Bonacorso HG, Cantos J, Carrion LL, Costa SS, Couto I, Fernandes LD, Junqueira E, Machado KS, Martins MA, Ramos DF, Seus VR, Silva L Jr, Viveiros M, von Groll A, Zanatta N
Publication Year: 2017
Journal: International Journal of Antimicrobial Agents
Link: http://www.ijaaonline.com/article/S0924-8579(17)30026-2/fulltext

The objectives of this study were to evaluate tetrahydropyridine derivatives as efflux inhibitors and to understand the mechanism of action of the compounds by in silico studies. Minimum inhibitory concentration (MIC) determination, fluorometric methods and docking simulations were performed. The compounds NUNL02, NUNL09 and NUNL10 inhibited efflux, and NUNL02 is very likely a substrate of […]
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Tetrahydropyridine derivative as efflux inhibitor in Mycobacterium abscessus

In silico and in vitro evaluation of tetrahydropyridine compounds as efflux inhibitors in Mycobacterium abscessus

In vitro and in silico analysis of the efficiency of tetrahydropyridines as drug efflux inhibitors in Escherichia coli

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