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Article

Identification of Novel Benzoxa-[2,1,3]-diazole Substituted Amino Acid Hydrazides as Potential Anti-Tubercular Agents

1
Institute for Cell and Molecular Biosciences, Faculty of Medical Sciences, Newcastle University, Catherine Cookson Building, Framlington Place, Newcastle upon Tyne NE2 4HH, UK
2
School of Pharmacy, Faculty of Medical Sciences, King George VI Building, Newcastle upon Tyne NE1 7RU, UK
3
Northern Institute for Cancer Research, Paul O′Gorman Building, Faculty of Medical Sciences, Newcastle University, Newcastle upon Tyne NE2 4HH, UK
4
Department of Chemistry, Durham University, Lower Mountjoy, Stockton Road, Durham DH1 3LE, UK
5
Chemistry, School of Natural and Environmental Sciences, Newcastle University, Newcastle upon Tyne NE1 7RU, UK
*
Author to whom correspondence should be addressed.
Academic Editor: Peter J. Rutledge
Molecules 2019, 24(4), 811; https://doi.org/10.3390/molecules24040811
Received: 29 January 2019 / Revised: 18 February 2019 / Accepted: 20 February 2019 / Published: 23 February 2019
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. View Full-Text
Keywords: benzoxa-[2,1,3]-diazole; antibacterial; Mycobacterium tuberculosis; amino acid; hydrazide benzoxa-[2,1,3]-diazole; antibacterial; Mycobacterium tuberculosis; amino acid; hydrazide
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MDPI and ACS Style

Brown, A.K.; Aljohani, A.K.B.; Gill, J.H.; Steel, P.G.; Sellars, J.D. Identification of Novel Benzoxa-[2,1,3]-diazole Substituted Amino Acid Hydrazides as Potential Anti-Tubercular Agents. Molecules 2019, 24, 811. https://doi.org/10.3390/molecules24040811

AMA Style

Brown AK, Aljohani AKB, Gill JH, Steel PG, Sellars JD. Identification of Novel Benzoxa-[2,1,3]-diazole Substituted Amino Acid Hydrazides as Potential Anti-Tubercular Agents. Molecules. 2019; 24(4):811. https://doi.org/10.3390/molecules24040811

Chicago/Turabian Style

Brown, Alistair K., Ahmed K. B. Aljohani, Jason H. Gill, Patrick G. Steel, and Jonathan D. Sellars. 2019. "Identification of Novel Benzoxa-[2,1,3]-diazole Substituted Amino Acid Hydrazides as Potential Anti-Tubercular Agents" Molecules 24, no. 4: 811. https://doi.org/10.3390/molecules24040811

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