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Autor:
Kavanagh, Madeline E, Coyne, Anthony G, McLean, Kirsty J, James, Guy G, Levy, Colin W, Marino, Leonardo B, de Carvalho, Luiz Pedro S, Chan, Daniel S H, Hudson, Sean A, Surade, Sachin, Leys, David, Munro, Andrew W, Abell, Chris
Publikováno v:
Journal of Medicinal Chemistry
Kavanagh, M E, Coyne, A G, McLean, K J, James, G G, Levy, C W, Marino, L B, de Carvalho, L P S, Chan, D S H, Hudson, S A, Surade, S, Leys, D, Munro, A W & Abell, C 2016, ' Fragment-Based Approaches to the Development of Mycobacterium tuberculosis CYP121 Inhibitors ', Journal of Medicinal Chemistry, vol. 59, no. 7, pp. 3272-302 . https://doi.org/10.1021/acs.jmedchem.6b00007
Kavanagh, M E, Coyne, A G, McLean, K J, James, G G, Levy, C W, Marino, L B, de Carvalho, L P S, Chan, D S H, Hudson, S A, Surade, S, Leys, D, Munro, A W & Abell, C 2016, ' Fragment-Based Approaches to the Development of Mycobacterium tuberculosis CYP121 Inhibitors ', Journal of Medicinal Chemistry, vol. 59, no. 7, pp. 3272-302 . https://doi.org/10.1021/acs.jmedchem.6b00007
The essential enzyme CYP121 is a target for drug development against antibiotic resistant strains of Mycobacterium tuberculosis. A triazol-1-yl phenol fragment 1 was identified to bind to CYP121 using a cascade of biophysical assays. Synthetic mergin