23269-52-5Relevant academic research and scientific papers
Design, synthesis, and antibacterial activity against rice bacterial leaf blight and leaf streak of 2,5-substituted-1,3,4-oxadiazole/thiadiazole sulfone derivative
Li, Pei,Shi, Li,Yang, Xia,Yang, Lei,Chen, Xue-Wen,Wu, Fang,Shi, Qing-Cai,Xu, Wei-Ming,He, Ming,Hu, De-Yu,Song, Bao-An
, p. 1677 - 1680 (2014/04/17)
A series of 2,5-substituted-1,3,4-oxadiazole/thiadiazole sulfone derivatives were synthesized and evaluated for their antibacterial activities against rice bacterial leaf blight and leaf streak caused by Xanthomonas oryzae pv. oryzae and Xanthomonas oryzae pv. oryzicolaby via the turbidimeter test in vitro. Antibacterial bioassay results indicated that most compounds demonstrated good inhibitory effect antibacterial bioactivities against rice bacterial leaf blight and leaf streak. Among the title compounds, compound 6c demonstrated the best inhibitory effect against rice bacterial leaf blight and leaf streak with half-maximal effective concentration (EC50) values of 1.07 and 7.14 μg/mL, respectively, which were even better than those of commercial agents such as Bismerthiazol and Thiediazole Copper. In vivo antibacterial activities tests at greenhouse conditions demonstrated that the controlling effect of compounds 6c (43.5%) and 6g (42.4%) against rice bacterial leaf blight were better than those of Bismerthiazol (25.5%) and Thiediazole Copper (37.5%).
A Novel Synthesis of Peptide Based on the Photochemistry of 5-Azido-1,3,4-oxadiazoles
Confalone, Pat N.,Woodward, Robert B.
, p. 902 - 906 (2007/10/02)
A novel approach to the synthesis of peptides is described.Various N-protected amino acid hydrazides 17 were converted to the salts 18 by condensation with carbon disulfide in methanolic potassium hydroxide.Thermal cyclization of 18 to the heterocycles 19 was followed by reaction with methyl iodide to yield the sulfides 20.After oxidation of 20 to the corresponding sulfones 21, the title compounds 22 were prepared by treating 21 with sodium azide.Deprotection then yielded the free bases 23.Utilization of 22 and 23 in peptide synthesis, relying on a photochemical degradation of the title heterocycle present in these compounds, is described.The scope and limitations of this new methodology are also discussed.
