Chinese Academy of Medical Sciences

Guangzhou Hc Pharmaceutical Co. Ltd

Institute of Medicinal Biotechnology, Chinese Academy of Medical

Xuefu You

Yang Chen

Yan Gao

Xi Lu

Yucheng Wang

Zhuorong Li

Mei Zhu

Sheng Tang

Jie Jin

Minghua Wang

Xiukun Wang

Yinghong Li

Xiaonan Du

Juxian Wang

Yanxiang Wang

Zhihao Guo

Zhiwen Li

Guoning Zhang

Danqing Song

Xinxin Hu

Along Cui

Qiyang He

The present invention relates to a compound as shown in general formula (I) below (in formula (I), each of Rand Rindependently represents a hydrogen atom or a C1-10 linear or branched alkyl optionally having a substituent, or the two together form a cycloalkyl with 3 to 8 ring carbon atoms; each of Rand Rindependently represents a hydrogen atom or a C1-10 linear or branched alkyl optionally having a substituent or a C6-12 aryl optionally having a substituent, or the two together form a cycloalkyl with 3 to 8 ring carbon atoms; X represents C or N; and Y represents a linear or branched alkenyl or alkynyl with 2 to 6 carbon atoms and optionally having a substituent, or carboxyl). The compound has good antibacterial properties against bacteria, especially gram-negative bacteria, has low drug resistance, and has good prospects for the effective treatment of various conditions.

β-lactam compound, use thereof and preparation method therefor

The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield.

Hydroxamic acid derivative, method for producing same and use thereof

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Beijing, China

Xuefu You