A Zn(Ⅱ) supramolecular coordination polymer, {[Zn2(L)2(m-bix)(H20)]6H2O}n(1), with an interesting 1D→2D polythreading array from a flexible and angular organic aromaticpolycarboxylate ligand 5-(4-hydroxyp...A Zn(Ⅱ) supramolecular coordination polymer, {[Zn2(L)2(m-bix)(H20)]6H2O}n(1), with an interesting 1D→2D polythreading array from a flexible and angular organic aromaticpolycarboxylate ligand 5-(4-hydroxypyridinium-l-ylmethyl)isophthalic acid (H2L), and N-donorligand 1,3-bis(imidazol-l-ylmethyl)benzene (m-bix), has been obtained under hydrothermalconditions and characterized by elemental analysis, powder X-ray diffraction (PXRD), IR, thermalgravimetric analyses (TGA) and single-crystal X-ray diffraction. In 1, the Zn(Ⅱ) center has twocoordination geometries. One exhibits a trigonal bipyramidal coordination sphere, and the other isa tetrahedral geometry; L2- has two different coordination modes, with one connecting three Zn(Ⅱ)ions through two monodentate carboxylate groups and the monodentate hydroxyl group, and theother bridging two Zn(Ⅱ) ions through two carboxylate groups. The L2- anions connect the Zn(Ⅱ)centers forming an infinite 1D tubular structure. These 1D tubes are interconnected by the m-bixspacers to form a 2D framework. Such 2D layers are further assembled into a 3D supramolecularnetwork via hydrogen bonds. Meanwhile, the luminescent property of 1 has also been investigatedin detail.展开更多
Abstract CC chemokine receptor 4 (CCR4) is a kind of G-protein-coupled receptor, which plays a pivotal role in allergic inflammation. The interaction between 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1- ylmethyl)-...Abstract CC chemokine receptor 4 (CCR4) is a kind of G-protein-coupled receptor, which plays a pivotal role in allergic inflammation. The interaction between 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1- ylmethyl)-carbamlyl]-methyl-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyi)-acetamide (S009) and the N-terminal extracellular tail (ML40) of CCR4 has been validated to be high affinity by capillary zone electrophoresis (CZE).The S009 is a known CCR4 antagonist. Now, a series of new thiourea derivatives have been synthesized. Compared with positive control S009, they were screened using ML40 as target by CZE to find some new drugs for allergic inflammation diseases. The synthesized compounds XJH-5, XJH-4, XJH-17 and XJH-1 displayed the interaction with ML40, but XJH-9, XJH-10, XJH-I 1, XJH-12, XJH-13, XJH-14, XJH-3, XJH-8, XJH-6, XJH-7, XJH-15, XJH-16 and XJH-2 did not bind to ML40. Both qualification and quantification characterizations of the binding were determined. The affinity of the four compounds was valued by the binding constant, which was similar with the results of chemotactic experiments. The established CEZ method is capable of sensitive and fast screening for a series of lactam analogs in the drug discovery for allergic inflammation diseases.展开更多
基金supported by Education Chamber of Henan Province(No.15A150068)
文摘A Zn(Ⅱ) supramolecular coordination polymer, {[Zn2(L)2(m-bix)(H20)]6H2O}n(1), with an interesting 1D→2D polythreading array from a flexible and angular organic aromaticpolycarboxylate ligand 5-(4-hydroxypyridinium-l-ylmethyl)isophthalic acid (H2L), and N-donorligand 1,3-bis(imidazol-l-ylmethyl)benzene (m-bix), has been obtained under hydrothermalconditions and characterized by elemental analysis, powder X-ray diffraction (PXRD), IR, thermalgravimetric analyses (TGA) and single-crystal X-ray diffraction. In 1, the Zn(Ⅱ) center has twocoordination geometries. One exhibits a trigonal bipyramidal coordination sphere, and the other isa tetrahedral geometry; L2- has two different coordination modes, with one connecting three Zn(Ⅱ)ions through two monodentate carboxylate groups and the monodentate hydroxyl group, and theother bridging two Zn(Ⅱ) ions through two carboxylate groups. The L2- anions connect the Zn(Ⅱ)centers forming an infinite 1D tubular structure. These 1D tubes are interconnected by the m-bixspacers to form a 2D framework. Such 2D layers are further assembled into a 3D supramolecularnetwork via hydrogen bonds. Meanwhile, the luminescent property of 1 has also been investigatedin detail.
基金supported by the National Key New Drug Creation Program of China (2009ZX09103-724)the National Natural Science Foundation of China grants(30872292,90813025 and 81072612)+2 种基金the Natural Science Foundation of Beijing (7102107)the Open Foundation of State Key Laboratory of Natural and Biomimetic Drugs(K20090207)the National New Drug Research and Development Project of China (2009ZX09301-010)
文摘Abstract CC chemokine receptor 4 (CCR4) is a kind of G-protein-coupled receptor, which plays a pivotal role in allergic inflammation. The interaction between 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1- ylmethyl)-carbamlyl]-methyl-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyi)-acetamide (S009) and the N-terminal extracellular tail (ML40) of CCR4 has been validated to be high affinity by capillary zone electrophoresis (CZE).The S009 is a known CCR4 antagonist. Now, a series of new thiourea derivatives have been synthesized. Compared with positive control S009, they were screened using ML40 as target by CZE to find some new drugs for allergic inflammation diseases. The synthesized compounds XJH-5, XJH-4, XJH-17 and XJH-1 displayed the interaction with ML40, but XJH-9, XJH-10, XJH-I 1, XJH-12, XJH-13, XJH-14, XJH-3, XJH-8, XJH-6, XJH-7, XJH-15, XJH-16 and XJH-2 did not bind to ML40. Both qualification and quantification characterizations of the binding were determined. The affinity of the four compounds was valued by the binding constant, which was similar with the results of chemotactic experiments. The established CEZ method is capable of sensitive and fast screening for a series of lactam analogs in the drug discovery for allergic inflammation diseases.