Design, synthesis and antimicrobial activities of thiouracil derivatives containing triazolo-thiadiazole as SecA inhibitors

作者：Cui, Penglei; Li, Xiaoliu^*; Zhu, Mengyuan; Wang, Binghe; Liu, Jing; Chen, Hua^*

来源：European Journal of Medicinal Chemistry, 2017, 127: 159-165.

DOI：10.1016/j.ejmech.2016.12.053

• Antibacterial activity
• SecA inhibitors
• Thiouracil
• Triazolo-thiadiazole
• Molecular simulation

A series of novel thiouracil derivatives containing a triazolo-thiadiazole moiety (7a-71) have been synthesized by structural modifications on a lead SecA inhibitor, 2. All the compounds have been evaluated for their antibacterial activities against Bacillus amyloliquefaciens, Staphylococcus aureus, and Bacillus subtilis. Compounds 7d and 7g were also tested for their inhibitory activities against SecA ATPase due to their promising antimicrobial activities. The inhibitory activity of compound 7d was found to be higher than that of 2. Molecular docking work suggests that compound 7d might bind at a pocket close to the ATPase ATP-binding domain.

• 出版日期2017-2-15
• 单位河北大学; 河北农业大学