文献类型：期刊文献

英文题名：Design, synthesis, and antibacterial activity of quinazolinone derivatives containing amides

作者：Zhang, Wenjuan Zhu, Yunying Zhang, Miaohe Mou, Honglan Wu, Rong Tang, Shouying Zhou, Han Luo, Jianlin Wei, Xian Feng, Shuang Bai, Song

第一作者：张文娟;Zhang, Wenjuan

通信作者：Feng, S[1];Bai, S[1];Bai, S[2];Bai, S[3]|[1444086c12c707ddfe99e]柏松;

机构：[1]Guizhou Inst Technol, Sch Chem Engn, Guiyang 550003, Peoples R China;[2]Guizhou Ind Polytech Coll, Guiyang 550008, Peoples R China;[3]Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 550025, Peoples R China

第一机构：贵州理工学院化学工程学院

通信机构：corresponding author), Guizhou Inst Technol, Sch Chem Engn, Guiyang 550003, Peoples R China;corresponding author), Guizhou Ind Polytech Coll, Guiyang 550008, Peoples R China;corresponding author), Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 550025, Peoples R China.|贵州理工学院化学工程学院;贵州理工学院;

年份：2023

卷号：56

起止页码：72-77

外文期刊名：PHYTOCHEMISTRY LETTERS

收录：;Scopus(收录号：2-s2.0-85164336877);WOS:【SCI-EXPANDED(收录号:WOS:001041161800001)】；

基金：The authors acknowledge support from the High School Science and Technology Talent Support Project of Guizhou Province, China (Qian Jiao He KY Zi [2021] 037) , the Science and Technology Planning Project of Guizhou Province (Qian Ke He Ji Chu ZK [2022] Zhong Dian 025) , High -Level Talent Initial Funding of Guizhou Institute of Technology (XJGC20190632) , the Earth Papers Project of Guizhou Institute of Technology (KJZX20-005) , the Opening Foundation of the Key Laboratory of Green Pesticide and Agricultural Bioengineering, the Ministry of Education, Guizhou University (Qian Jiao Ji [2022] 433) , the Young Science and Technology Talent Development Program of Education Department of Guizhou Province (Qian Jiao He KY Zi [2022] 346 Hao) , the Academic New Seedling Cultivation and Exploration and Innovation Project of Guizhou Institute of Technology (GZLGXM-03 & GZLGXM- 14 & GZLGXM-20) , the Science and Technology Program of Guizhou Province (Qian Ke He Ji Chu [2019] 1139) , the Young Science and Technology Talent Development Program of Education Department of Guizhou Province (Qian Jiao He KY Zi [2018] 251) , the Opening Foundation of the Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University (Qian Jiao He KY Zi [2018] 472) , and the Opening Foundation of the Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University (No. 2018GDGP0102) . We thank LetPub ( www.letpub.com ) for its linguistic assistance during the preparation of this manuscript.

语种：英文

外文关键词：Quinazolinone derivatives; Biological activity; Xanthomonas oryzae pv; oryzae; Pseudomonas syringae pv; actinidiae

摘要：In this study, a series of new quinazolinone derivatives containing amides was designed and synthesized using the principle of active splicing. These compounds were tested for their biological activity and found to possess some antibacterial activity. Among these, compound 18 showed good activity against Pseudomonas syringae pv. actinidiae (Psa) in vitro with an EC50 value of 39.2 mg/L, which was superior to thiodiazole copper (73.9 mg/L) and zinc thiazole (45.1 mg/L). Compound 18 also showed good antibacterial activity against Xanthomonas oryzae pv. oryzae (Xoo) in vitro at 100 mg/L, with an inhibition rate of 70.9 %, which was superior to thiodiazole copper (68.5 %) and zinc thiazole (70.2 %). According to the structure-activity relationship analysis, different R1 positions or the incorporation of an electron donor substituent greatly affected the antibacterial activity of the compounds. Following scanning electron microscopy experiments, compound 18 was found to cause fragmentation and surface wrinkling of the bacteria, leading to an antibacterial effect. Therefore, compound 18 may be further optimized, providing a foundation as a potential antibacterial agent.