1155869-00-3Relevant academic research and scientific papers
Novel 4H-1,3,4-oxadiazin-5(6H)-ones with hydrophobic and long alkyl chains: Design, synthesis, and bioactive diversity on inhibition of monoamine oxidase, chitin biosynthesis and tumor cell
Ke, Shao-Yong,Qian, Xu-Hong,Liu, Feng-Yi,Wang, Ni,Yang, Qing,Li, Zhong
experimental part, p. 2113 - 2121 (2009/10/02)
A new series of nitrogen-containing heterocycles 4H-1,3,4-oxadiazin-5(6H)-ones derivatives with hydrophobic and long chains were designed and synthesized by direct cyclization reaction of N′-alkylation substituted aroylhydrazines with chloroacetyl chloride. The preliminary assays showed that some of the compounds displayed moderate to good inhibitory activities toward monoamine oxidase (MAO) at the concentration of 10-5-10-3 M, and antitumor activities against human lung cancer A-549 and human prostate cancer PC-3 cell lines at μM level, which might provide new scaffold for anticancer agents. Furthermore, compounds 5i and 5m exhibited significant inhibitory activity on chitin biosynthesis, which might represent a novel class of highly potential inhibitors of chitin synthesis. Crown Copyright
Diacylhydrazine derivatives as novel potential chitin biosynthesis inhibitors: Design, synthesis, and structure-activity relationship
Ke, Shaoyong,Qian, Xuhong,Liu, Fengyi,Wang, Ni,Fan, Feng,Li, Zhong,Yang, Qing
experimental part, p. 2985 - 2993 (2009/10/02)
A series of diacylhydrazine derivatives containing hydrophobic alkyl chains have been designed and synthesized. The target molecules have been identified on the basis of analytical spectral (IR, 1H NMR, 13C NMR, and HRMS) data. All synthesized compounds have been screened for their potential inhibition in vitro against chitin synthesis using yeast cell extracts. The preliminary assays indicate that some of the compounds display moderate to good inhibitory activity. Structure-activity relationship (SAR) is also discussed based on the experimental data, and the further analysis of the quantitative structure-activity relationship (QSAR) indicates that the electronic parameter is the main factor to affect inhibition activities.
1,3,4-Oxadiazoline derivatives as novel potential inhibitors targeting chitin biosynthesis: Design, synthesis and biological evaluation
Ke, Shaoyong,Liu, Fengyi,Wang, Ni,Yang, Qing,Qian, Xuhong
scheme or table, p. 332 - 335 (2011/02/26)
Two series of 1,3,4-oxadiazoline heterocycle derivatives were designed, synthesized and identified. Bioactivity assays showed that all synthesized compounds inhibited chitin synthesis in yeast, suggesting they might be a novel class of potential inhibitors against chitin biosynthesis. The structure-activity relationships (SAR) of these compounds are discussed.
