Design, Synthesis, and Evaluation of Thiol-Activated Sources of Sulfur Dioxide (SO2) as Antimycobacterial Agents

作者：Malwal Satish R; Sriram Dharmarajan; Yogeeswari Perumal; Konkimalla V Badireenath; Chakrapani Harinath^*

来源：Journal of Medicinal Chemistry, 2012, 55(1): 553-557.

DOI：10.1021/jm201023g

Here, 2,4-dinitrophenylsulfonamides with tunable cysteine-activated SO2 release profiles with half-lives of SO2 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 mu M) of inhibiting Mycobacterium tuberculosis (Mtb) higher than the clinical agent isoniazid (MIC = 0.37 mu M).

• 出版日期2012-1-12