An evaluation of Minor Groove Binders as anti-fungal and anti-mycobacterial therapeutics

Scott, F. J. et al. (2017) An evaluation of Minor Groove Binders as anti-fungal and anti-mycobacterial therapeutics. European Journal of Medicinal Chemistry, 136, pp. 561-572. (doi: 10.1016/j.ejmech.2017.05.039)

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This study details the synthesis and biological evaluation of a collection of 19 structurally related Minor Groove Binders (MGBs), derived from the natural product distamycin, which were designed to probe antifungal and antimycobacterial activity. From this initial set, we report several MGBs that are worth more detailed investigation and optimisation. MGB-4, MGB-317 and MGB-325 have promising MIC80s of 2, 4 and 0.25 μg/mL, respectively, against the fungus C. neoformans.MGB-353 and MGB-354 have MIC99s of 3.1 μM against the mycobacterium M. tuberculosis. The selectivity and activity of these compounds is related to their physicochemical properties and the cell wall/membrane characteristics of the infective agents.

Item Type:Articles
Glasgow Author(s) Enlighten ID:Khalaf, Dr Abedawn and Giordani, Dr Federica and Barrett, Professor Michael
Authors: Scott, F. J., Nichol, R. J.O., Khalaf, A. I., Giordani, F., Gillingwater, K., Ramu, S., Elliott, A., Zuegg, J., Duffy, P., Rosslee, M.-J., Hlaka, L., Kumar, S., Ozturk, M., Brombacher, F., Barrett, M., Guler, R., and Suckling, C. J.
College/School:College of Medical Veterinary and Life Sciences > School of Infection & Immunity
College of Science and Engineering > School of Chemistry
Journal Name:European Journal of Medicinal Chemistry
ISSN (Online):1768-3254
Published Online:17 May 2017
Copyright Holders:Copyright © 2017 Elsevier Masson SAS
First Published:First published in European Journal of Medicinal Chemistry 136:561-572
Publisher Policy:Reproduced in accordance with the copyright policy of the publisher

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