期刊
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
卷 194, 期 3, 页码 241-248出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/10426507.2018.1539992
关键词
Benzothiazole; 1; 3; 4-thiadiazole; antibacterial activity; antifungal activity; antiviral activity
资金
- National Key Research and Development Program of China [2017YFD0200506]
- National Nature Science Foundation of China [21867003]
- Major Program of Innovation Research Team of Educational Commission of Guizhou Province [2016113]
- Science and Technology Platform for Talent of Guizhou Province [20165608]
- Science and Technology Project of Guizhou Province [20172956]
A series of benzothiazole derivatives bearing a 1,3,4-thiadiazole moiety were designed, synthesized and evaluated for their antibacterial, antifungal and antiviral activities. The bioassay results indicated that most of target compounds showed good antiviral activities against tobacco mosaic virus (TMV) and antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Ralstonia solanacearum (Rs). Especially, the anti-Xoo effect of title compounds 5k (N-(5-methoxybenzo[d]thiazol-2-yl)-2-((5-(2-tolyl)-1,3,4-thiadiazol-2-yl)thio)acetamide) and the anti-Rs effect of title compounds 5a (N-(5-nitrobenzo[d]thiazol-2-yl)-2-((5-(4-(trifluorom ethyl)phenyl)-1,3,4-thiadiazol-2-yl)thio)acetmide) respectively reached 52.4% and 71.6% at 100 mu g/mL, which are superior to that of bismerthiazol (32.0% and 52.3%). In addition, the protective and inactivation activities of title compound 5i (N-(5-methoxybenzo [d]thiazol-2-yl)-2-((5-(4-nitrophenyl)-1,3,4-thiadiazol-2-yl)thio)acetamide) against TMV were 79.5% and 88.3%, respectively, which are better than that of ningnanmycin (76.4% and 86.8%). The above research showed that benzothiazole derivatives bearing a 1,3,4-thiadiazole moiety may be used as potential molecular templates in searching for highly-efficient antiviral and antibacterial agents.
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