Publications
Chosen filters:
Chosen filters:
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors Vrije Universiteit Brussel
Mycobacterial transcriptional repressor EthR controls the expression of EthA, the bacterial monooxygenase activating ethionamide, and is thus largely responsible for the low sensitivity of the human pathogen Mycobacterium tuberculosis to this antibiotic. We recently reported structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors leading to the discovery of potent ethionamide boosters. Despite high metabolic stability, ...
Discovery of novel N -phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis Vrije Universiteit Brussel
In this paper, we describe the screening of a 14640-compound library using a novel whole mycobacteria phenotypic assay to discover inhibitors of EthR, a transcriptional repressor implicated in the innate resistance of Mycobacterium tuberculosis to the second-line antituberculosis drug ethionamide. From this screening a new chemical family of EthR inhibitors bearing an N-phenylphenoxyacetamide motif was identified. The X-ray structure of the most ...
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity. Flanders Institute for Biotechnology Vrije Universiteit Brussel
Development and Validation of a Fast Reversed Phase Liquid Chromatographic Method for the Analysis of Ethionamide in Dosage Forms KU Leuven
© 2018, Bentham Science Publishers B.V. All rights reserved. Background: Ethionamide (ETA) is widely used as one of the agents for the treatment of multidrug resistant tuberculosis. Although quality control is an important issue, a fast LC-UV method for the assay and impurity determination of ETA was lacking. So, the aim of this study was to develop such a method to evaluate drug products and follow up dissolution tests of ETA tablets. Methods: ...
Sensibilité envers la dapsone, la sulfamethoxypyridazine et l'éthionamide, de Mycobacterium leprae provenant de malades traités par ces substances Institute of Tropical Medicine
Synthesis and properties of hydrazones bearing amide, thioamide and amidine functions KU Leuven
This review provides detailed methods for the synthesis, structures and chemical properties of hydrazones bearing carboxamide, thioamide and amidine functions. The main accent was put on the cyclization reactions leading to pyrazoles, thiazoles, 1,2,3-triazoles, 1,2,3-thiadiazoles, 1,2,4-triazines and other heterocyclic compounds. In addition, we have reviewed methods for the synthesis of substrates for pericyclic reactions from the hydrazones.
Hepatotoxicity of the combination of rifampin-ethionamide in the treatment of multibacillary leprosy Institute of Tropical Medicine
Management of multidrug-resistant tuberculosis with shorter treatment regimen in Niger: nationwide programmatic achievements Institute of Tropical Medicine
Background: In Niger, the Shorter Treatment Regimen (STR) has been implemented nationwide for rifampicin resistant tuberculosis (RR-TB), since 2008. No previous publication has shown the results from countrywide programmatic implementation using few exclusion criteria, nor exhaustively assessed the effect of initial resistance to companion drugs on outcomes.
Methods: The National Tuberculosis Programme and the Damien Foundation ...