Brown, Alistair and Aljohani, Ahmed and Gill, Jason and Steel, Patrick and Sellars, Jonathan (2019) 'Identification of novel benzoxa-[2,1,3]-diazole substituted amino acid hydrazides as potential anti-tubercular agents.', Molecules., 24 (4). p. 811.
Discovery and development of new therapeutic options for the treatment of Mycobacterium tuberculosis (Mtb) infection are desperately needed to tackle the continuing global burden of this disease and the efficacy and cost limitations associated with current medicines. Herein, we report the synthesis of a series of novel benzoxa-[2,1,3]-diazole substituted amino acid hydrazides in a two-step synthesis and evaluate their inhibitory activity against Mtb and selected bacterial strains of clinical importance utilising an end point-determined REMA assay. Alongside this, their potential for undesired cytotoxicity against mammalian cells was assessed employing standard MTT assay methodologies. It has been demonstrated using modification at three sites (the hydrazine, amino acid, and the benzodiazole) it is possible to change both the antibacterial activity and cytotoxicity of these molecules whilst not affecting their microbial selectivity, making them attractive architectures for further exploitation as novel antibacterial agents.
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|Publisher Web site:||https://doi.org/10.3390/molecules24040811|
|Publisher statement:||© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).|
|Date accepted:||20 February 2019|
|Date deposited:||07 March 2019|
|Date of first online publication:||23 February 2019|
|Date first made open access:||07 March 2019|
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