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- * Among these MGBs, MGB-4, MGB-317, and MGB-325 showed strong activity against the fungus C. neoformans, with minimum inhibitory concentrations (MICs) of 2, 4, and 0.25 μg/mL, respectively.
- * MGB-353 and MGB-354 also displayed good potential against M. tuberculosis, with MICs of 3.1 μM, indicating that their effectiveness is linked to their chemical properties and the characteristics of the
Article 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 MICs of 2, 4 and 0.25 μg/mL, respectively, against the fungus C. neoformans.MGB-353 and MGB-354 have MICs 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.
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| http://dx.doi.org/10.1016/j.ejmech.2017.05.039 | DOI Listing |
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