Design, Synthesis, and Evaluation of Thiol-Activated Sources of Sulfur Dioxide (SO2) as Antimycobacterial Agents
Journal of Medicinal Chemistry2011Vol. 55(1), pp. 553–557
Citations Over TimeTop 10% of 2011 papers
Satish R. Malwal, Dharmarajan Sriram, Perumal Yogeeswari, V. Badireenath Konkimalla, Harinath Chakrapani
Abstract
Here, 2,4-dinitrophenylsulfonamides with tunable cysteine-activated SO(2) release profiles with half-lives of SO(2) release varying from 2 to 63 min are reported. N-Benzyl-2,4-dinitrobenzenesulfonamide (6), which is prepared in one step from commercial sources, had a potency (MIC = 0.15 μM) of inhibiting Mycobacterium tuberculosis (Mtb) higher than the clinical agent isoniazid (MIC = 0.37 μM).
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