摘要
Two new 5-alkylpyrrole-2-carboxaldehyde derivatives,mycalenitrile-15（1） and mycalenitrile-16（2）,along with five known related ones（3-7）,were isolated from the South China Sea sponge Mycale lissochela.The structures of the new compounds were elucidated on the basis of extensive spectroscopic analysis and by comparison of their NMR data with those reported in the literature.In bioassay,compounds 1 and 7 exhibited significant PTPIB（Protein-tyrosine phosphatase 1B,a recognized target for diabetes and obesity） inhibitory activities with IC（50） values of 8.6 and 3.1 μmoI/L,respectively.A preliminary SAR analysis of the isolated compounds with their PTP1 B inhibitory effects was described.
Two new 5-alkylpyrrole-2-carboxaldehyde derivatives,mycalenitrile-15（1） and mycalenitrile-16（2）,along with five known related ones（3-7）,were isolated from the South China Sea sponge Mycale lissochela.The structures of the new compounds were elucidated on the basis of extensive spectroscopic analysis and by comparison of their NMR data with those reported in the literature.In bioassay,compounds 1 and 7 exhibited significant PTPIB（Protein-tyrosine phosphatase 1B,a recognized target for diabetes and obesity） inhibitory activities with IC（50） values of 8.6 and 3.1 μmoI/L,respectively.A preliminary SAR analysis of the isolated compounds with their PTP1 B inhibitory effects was described.
基金
financially supported by the National Natural Science Foundation of China(Nos.41476063,81520108028,81273430,41306130 81302692,41676073,81603022)
SCTSM Project from Shanghai Science and Technology Committee,Shanghai,China(Nos.14431901100,15431901000)
The project from Institutes for Drug Discovery and Development,Chinese Academy of Sciences,China(No.CASIMM0120152039)
the SKLDR/SIMM Projects from Shanghai Institute of MateriaMedica,China(No.SIMM 1501ZZ-03)
support of "Youth Innovation Promotion Association"(No.2016258) from Chinese Academy of Sciences
"Young Talent Supporting Project" from China Association for Science and Technology(No.2016QNRC001)
Shanghai "Pujiang Program"(No.16PJ1410600)
