Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase.
作者信息
Nicholas Gillian M, Eckman Lisa L, Ray Satyajit, Hughes Robert O, Pfefferkorn Jeffrey A, Barluenga Sofia, Nicolaou K C, Bewley Carole A
机构信息
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0820, USA.
出版信息
Bioorg Med Chem Lett. 2002 Sep 2;12(17):2487-90. doi: 10.1016/s0960-894x(02)00385-2.
A series of bromotyrosine-derived compounds, including marine natural products and members of a psammaplin A-inspired combinatorial synthetic library, were screened for their ability to inhibit the Mycobacterium tuberculosis detoxification enzyme mycothiol-S-conjugate amidase (MCA). Correlations between the structures and their respective IC(50) values (which range from 3 microM to 2.7 mM) should prove valuable when optimizing more potent inhibitors of MCA.
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