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

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• 作者：Satish R. Malwal ; Dharmarajan Sriram ; Perumal Yogeeswari ; V. Badireenath Konkimalla ; Harinath Chakrapani
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：January 12, 2012
• 年：2012
• 卷：55
• 期：1
• 页码：553-557
• 全文大小：245K
• 年卷期：v.55,no.1(January 12, 2012)
• ISSN：1520-4804

文摘

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 渭M) of inhibiting Mycobacterium tuberculosis (Mtb) higher than the clinical agent isoniazid (MIC = 0.37 渭M).