Synthesis and antibacterial evaluation of new monobactams

Zaw Min Thu; Jian Sun; Jingwen Ji; Lili He; Jinbo Ji; Zafar Iqbal; Ko Ko Myo; Yuanyu Gao; Lijuan Zhai; Yangxiu Mu; Dong Tang; Giovanni Vidari; Haikang Yang; Zhixiang Yang

doi:10.1016/j.bmcl.2021.127878

Synthesis and antibacterial evaluation of new monobactams

Bioorg Med Chem Lett. 2021 May 1:39:127878. doi: 10.1016/j.bmcl.2021.127878. Epub 2021 Feb 24.

Authors

Zaw Min Thu¹, Jian Sun², Jingwen Ji², Lili He², Jinbo Ji², Zafar Iqbal², Ko Ko Myo¹, Yuanyu Gao², Lijuan Zhai², Yangxiu Mu², Dong Tang², Giovanni Vidari³, Haikang Yang⁴, Zhixiang Yang⁵

Affiliations

¹ Ningxia Centre of Organic Synthesis and Engineering Technology, Ningxia Academy of Agriculture and Forestry Sciences, No. 590, Huanghe East Road, Jinfeng District, Yinchuan, Ningxia 750002, PR China; Department of Chemistry, Kalay University, Kalay 03044, Sagaing Region, Myanmar.
² Ningxia Centre of Organic Synthesis and Engineering Technology, Ningxia Academy of Agriculture and Forestry Sciences, No. 590, Huanghe East Road, Jinfeng District, Yinchuan, Ningxia 750002, PR China.
³ Medical Analysis Department, Faculty of Science, Tishk International University, Erbil 44001, Kurdistan Region, Iraq.
⁴ Ningxia Centre of Organic Synthesis and Engineering Technology, Ningxia Academy of Agriculture and Forestry Sciences, No. 590, Huanghe East Road, Jinfeng District, Yinchuan, Ningxia 750002, PR China. Electronic address: yhk777@yahoo.com.
⁵ Ningxia Centre of Organic Synthesis and Engineering Technology, Ningxia Academy of Agriculture and Forestry Sciences, No. 590, Huanghe East Road, Jinfeng District, Yinchuan, Ningxia 750002, PR China. Electronic address: yangzhixiang8@163.com.

PMID: 33636305
DOI: 10.1016/j.bmcl.2021.127878

Abstract

Monobactams play an important role in antibiotic drug discovery. Based on the structural characteristics of aztreonam and its biological targets, six new monobactam derivatives (2a-c and 3a-c) were synthesized and their in vitro antibacterial activities were investigated. Compounds 2a-c showed higher activities against tested gram-negative bacteria than that of parent aztreonam. Monobactam 2c exhibited the most potent activities, with MIC ranging from 0.25 to 2 μg/mL against most bacteria.

Keywords: Antibacterial; Aztreonam; Gram-negative; Monobactam.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Dose-Response Relationship, Drug
Gram-Negative Bacteria / drug effects*
Microbial Sensitivity Tests
Molecular Structure
Monobactams / chemical synthesis
Monobactams / chemistry
Monobactams / pharmacology*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Monobactams