期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 70, 期 20, 页码 6050-6058出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jafc.2c01407
关键词
axial chirality; thiazine; atropisomer; antibacterial; Xoo
资金
- National Natural Science Foundation of China [21772029, 32172459, 21961006, 22071036]
- 10 Talent Plan (Shicengci) of Guizhou Province [[2016]5649]
- Science and Technology Department of Guizhou Province [[2019]1020, ZK[2021]Key033]
- Program of Introducing Talents of Discipline to Universities of China (111 Program) at Guizhou University, Frontiers Science Center for Asymmetric Synthesis and Medicinal Molecules [D20023]
- Department of Education, Guizhou Province [Qianjiaohe KY (2020)004]
- Guizhou Province First-Class Disciplines Project [GNYL(2017)008]
- Guizhou University of Traditional Chinese Medicine, and Guizhou University (China)
- Singapore National Research Foundation under its NRF Investigatorship [NRF-NRFI2016-06]
- Competitive Research Program [NRF-CRP22-2019-0002]
- Ministry of Education, Singapore [RG7/20, RG5/19, MOE2019-T2-2-117, MOE2018-T3-1-003]
- Nanyang Research Award Grant, Chair Professorship Grant, Nanyang Technological University
A new class of axially chiral thiazine molecules were constructed and showed promising antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo). The axial chiralities of these compounds had clear impacts on the inhibitory activities against Xoo. The optimal molecule exhibited superior inhibitory activity and outperformed the controls in in vivo studies.
A new class of axially chiral thiazine molecules were constructed and showed promising antibacterial activities againstthe plant pathogenXanthomonas oryzaepv.oryzae(Xoo). The axial chiralities of these compounds (R-orS-atropisomer) showedclear impacts on the in vitro inhibitory activities againstXoo. An optimal molecule of this class with the (S)-axially chiralconfiguration was identified to exhibit inhibitory activity againstXoowith an EC50value of 4.18 mu g/mL. This inhibition efficiency issuperior to that of two commercial antibacterial agrochemicals, thiodiazole-copper and bismerthiazol, as the positive controls. Thishit compound also performed better than the controls in our in vivo studies. Preliminary mechanistic studies via scanning electronmicroscopy images showed that our hit compound at a concentration of 10 mu g/mL destroyed the bacterial integrity ofXoo. Label-free quantitative proteomics analysis indicated that a total of 366 differentially expressed proteins of the rice plants were significantlyinfluenced in the presence of our hit molecule.
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