Preparation, antibacterial evaluation and preliminary structure–activity relationship (SAR) study of benzothiazol-and benzoxazol-2-amine derivatives

L Ouyang, Y Huang, Y Zhao, G He, Y Xie, J Liu…

Index: Ouyang, Liang; Huang, Yuhui; Zhao, Yuwei; He, Gu; Xie, Yongmei; Liu, Jie; He, Jun; Liu, Bo; Wei, Yuquan Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 9 p. 3044 - 3049

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Citation Number: 25

Abstract

In this study, a novel benzothiazol-and benzooxazol-2-amine scaffold with antibacterial activity was designed and synthesized. Preliminary structure–activity relationship analysis displayed that compound 8t with a 5, 6-difluorosubstituted benzothiazole was found to be a potent inhibitor of Gram-positive pathogens, and exhibited some potential against drug- resistant bacteria and without cytotoxicity in therapeutic concentrations. In addition, ...