3H-1, 2, 4-Dithiazol-3-one compounds as novel potential affordable antitubercular agents

…, L Xiong, W Ang, T Yang, J He, Y Liu, Y Chang…

Index: Yang, Jianzhong; Pi, Weiyi; Xiong, Li; Ang, Wei; Yang, Tao; He, Jun; Liu, Yuanyuan; Chang, Ying; Ye, Weiwei; Wang, Zhenling; Luo, Youfu; Wei, Yuquan Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 5 p. 1424 - 1427

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Abstract

Small molecules with oxathiazol-2-one moiety were recently reported as potent inhibitors of Mycobacterium bovis var. bacilli Calmette–Guérin (BCG), among which HT1171 was the most potent and selective proteasome inhibitor. Herein we synthesized a series of novel compounds by bioisosteric replacement of the oxathiazol-2-one ring with 3H-1, 2, 4-dithiazol- 3-one, and also fifteen 1, 3, 4-oxathiazol-2-one molecules in order for potency comparison ...