Title |
An evaluation of Minor Groove Binders as anti-fungal and anti-mycobacterial therapeutics
|
---|---|
Published in |
European Journal of Medicinal Chemistry, May 2017
|
DOI | 10.1016/j.ejmech.2017.05.039 |
Pubmed ID | |
Authors |
Fraser J. Scott, Ryan J.O. Nichol, Abedawn I. Khalaf, Federica Giordani, Kirsten Gillingwater, Soumya Ramu, Alysha Elliott, Johannes Zuegg, Paula Duffy, Michael-Jon Rosslee, Lerato Hlaka, Santosh Kumar, Mumin Ozturk, Frank Brombacher, Michael Barrett, Reto Guler, Colin J. Suckling |
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. |
X Demographics
Geographical breakdown
Country | Count | As % |
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United Kingdom | 4 | 67% |
Unknown | 2 | 33% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 4 | 67% |
Scientists | 2 | 33% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Unknown | 44 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Master | 9 | 20% |
Researcher | 7 | 16% |
Student > Ph. D. Student | 5 | 11% |
Student > Bachelor | 3 | 7% |
Student > Doctoral Student | 3 | 7% |
Other | 8 | 18% |
Unknown | 9 | 20% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 15 | 34% |
Medicine and Dentistry | 7 | 16% |
Immunology and Microbiology | 3 | 7% |
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 5% |
Biochemistry, Genetics and Molecular Biology | 2 | 5% |
Other | 3 | 7% |
Unknown | 12 | 27% |