Quinoline derivatives were efficiently prepared through acid-catalyzed Friedlander reaction in ionic liquid ([bmim][BF4]). It is shown that the proposed method is operationally simple and environmentally benign in tha...Quinoline derivatives were efficiently prepared through acid-catalyzed Friedlander reaction in ionic liquid ([bmim][BF4]). It is shown that the proposed method is operationally simple and environmentally benign in that the reaction media and the catalyst can be recovered and be reused effectively for at least four times.展开更多
Insect chitinolyticβ-N-acetyl-D-hexosaminidase,such as OfHex1 from Ostrinia furnacalis,is a potential target for insecticide design.Among the known OfH ex1 inhibitors,Q2 is of great interest because it is the first n...Insect chitinolyticβ-N-acetyl-D-hexosaminidase,such as OfHex1 from Ostrinia furnacalis,is a potential target for insecticide design.Among the known OfH ex1 inhibitors,Q2 is of great interest because it is the first non-carbohydrate inhibitor.In this study,we designed and synthesized a series of Q2 derivatives by replacing the thiadiazole and naphthalimide groups and changing the linker length.Compound 3 m showed the best inhibitory activity with a Kivalue of 0.34 mmol/L against OfHex1,which is about onequarter that of Q2(K_i=1.4 mmol/L).Compound 6 a showed the best inhibitory activity among the quinoline-containing derivatives(K_i=2.3 mmol/L).Molecular docking indicated that although 3 m,6 a,and Q2 binding the active pocket of OfHex1 in similar mode,compound 3 m engaged better than the other compounds in intermolecular interaction with OfH ex1.展开更多
文摘Quinoline derivatives were efficiently prepared through acid-catalyzed Friedlander reaction in ionic liquid ([bmim][BF4]). It is shown that the proposed method is operationally simple and environmentally benign in that the reaction media and the catalyst can be recovered and be reused effectively for at least four times.
基金the National Key Research and Development Program of China(Nos.2017YFD0200500,2017YFD0201400,2018YFD0200100)the National Natural Science Foundation of China(No.31871959)for the financial support
文摘Insect chitinolyticβ-N-acetyl-D-hexosaminidase,such as OfHex1 from Ostrinia furnacalis,is a potential target for insecticide design.Among the known OfH ex1 inhibitors,Q2 is of great interest because it is the first non-carbohydrate inhibitor.In this study,we designed and synthesized a series of Q2 derivatives by replacing the thiadiazole and naphthalimide groups and changing the linker length.Compound 3 m showed the best inhibitory activity with a Kivalue of 0.34 mmol/L against OfHex1,which is about onequarter that of Q2(K_i=1.4 mmol/L).Compound 6 a showed the best inhibitory activity among the quinoline-containing derivatives(K_i=2.3 mmol/L).Molecular docking indicated that although 3 m,6 a,and Q2 binding the active pocket of OfHex1 in similar mode,compound 3 m engaged better than the other compounds in intermolecular interaction with OfH ex1.
