| Literature DB >> 28544982 |
Fraser J Scott1, Ryan J O Nichol2, Abedawn I Khalaf2, Federica Giordani3, Kirsten Gillingwater4, Soumya Ramu5, Alysha Elliott5, Johannes Zuegg5, Paula Duffy2, Michael-Jon Rosslee6, Lerato Hlaka6, Santosh Kumar6, Mumin Ozturk6, Frank Brombacher6, Michael Barrett3, Reto Guler6, Colin J Suckling2.
Abstract
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.Entities:
Keywords: Anti-infective; Anti-tuberculosis; Antifungal; Minor Groove Binders
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Year: 2017 PMID： 28544982 DOI： 10.1016/j.ejmech.2017.05.039
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514