The carcinogenic antioxidants,N-phenyl-1-naphthylamine (P1NA)and N-phenyl-2-naphthylamine (P2NA) were examined in vitro for biotransformation by rat hepatic microsomes and in freshly isolated hepatocytes. HPLC-analysi...The carcinogenic antioxidants,N-phenyl-1-naphthylamine (P1NA)and N-phenyl-2-naphthylamine (P2NA) were examined in vitro for biotransformation by rat hepatic microsomes and in freshly isolated hepatocytes. HPLC-analysis of hepatocyte incubations with revealed that phenols were the major metabolites in both cases. P1NA formed one phenolic metabolite only, while incubation with P2NA yielded two phenols identified as 6-hydroxy-P2NA and 4'-hydroxy-P2NA by cochromatography with authentic samples. β-naphthylamine, a metabolite indicating dephenylation of P2NA was not detectable.Metabolism studies with microsomes revealed that the phenols were formed by cytochrome P-450 dependent monooxygenases. Pretreatment of animals with phenobarbital and 3-methylcholanthrene both increased the rate of microsomal metabolism of P1NA and P2NA, indicating that more than one P-450 enzyme mediate the oxygenation reaction. Animal pretreatment with single and repeated doses of P1NA and P2NA did not markedly stimulate metabolism, but induced ethylmorphine demethylatior. in males and females and benzo (a)pyrene hydroxylation in females.展开更多
The title compound N-phenyl-2-deoxy-D-ribopyranosylamine featuring a single conformation and pyranose-ring has been synthesized and characterized by NMR spectrum and X-ray diffraction. X-ray crystal structure analysis...The title compound N-phenyl-2-deoxy-D-ribopyranosylamine featuring a single conformation and pyranose-ring has been synthesized and characterized by NMR spectrum and X-ray diffraction. X-ray crystal structure analysis shows that its crystal belongs to the monoclinic system, space group P21 with a = 6.5375(9), b = 7.7140(9), c = 10.7865(16)A, β= 97.578(11)^o, Z = 2, V= 539.22(13)A^3, Dc = 1.289 g/cm^3, F(000) = 224, μ(MoKa) --- 4.533 mm^-1, R = 0.0305 and wR = 0.0639 for 1093 observed reflections (I 〉 2σ(I). This compound exists as a-conformation and ^1C4 chair-like configuration.展开更多
Thirteen novel N-(2-fluoro-5-(3-methyl-2,6-dioxo-4-(trifluoromethy)-2,3-dihydropyrimidin-1(6H)-yl)phenyl)- 2-phenoxy)acetamides were designed and synthesized utilizing 4-fluoro-aniline and ethyl 3-amino-4,4,4...Thirteen novel N-(2-fluoro-5-(3-methyl-2,6-dioxo-4-(trifluoromethy)-2,3-dihydropyrimidin-1(6H)-yl)phenyl)- 2-phenoxy)acetamides were designed and synthesized utilizing 4-fluoro-aniline and ethyl 3-amino-4,4,4-trifluoro-but-2-enoate as starting materials. The chemical structures of all compounds were confirmed by IH NMR, IR, mass spectrum and elemental analyses. Subsequently, the herbicidal activities of the as-prepared compounds were evalu-ated in the greenhouse. Bioassay results indicated that most of compounds had better herbicidal activities against dicotyledonous weeds. Among all the tested compounds, compounds 4a--4i showed good herbicidal activities at both pre-emergence and post-emergence treatment against two or three kinds of dicotyledonous weeds, such as Abutilon theophrasti Medic, Amaranthus ascendens L, and Chenopodium album L at the dosage of 75 g ai/ha.展开更多
Three complexes Cu(ppca)2(H2O)2(NO3)2 (1), Cu2(μ-OH)2(ppca)2(H2O)4)·(ClO4)2 (2) and Cu2(μ-CH3COO)4(ppca)2(3) have been synthesized by the reaction of copper(Ⅱ) salts with N-phenyl-4-...Three complexes Cu(ppca)2(H2O)2(NO3)2 (1), Cu2(μ-OH)2(ppca)2(H2O)4)·(ClO4)2 (2) and Cu2(μ-CH3COO)4(ppca)2(3) have been synthesized by the reaction of copper(Ⅱ) salts with N-phenyl-4-pyridinecarboxamide (ppca) and characterized. For anions, in complex 1, NO3^- coordinated with copper(Ⅱ), in complex 2 perchlorate anion did not take part in coordination, the copper(Ⅱ) cations were connected by μ-OH to form a dinuclear unit, and complex 3 had a dimeric copper(Ⅱ) carboxylate paddle-wheel core. Noncovalent interactions linked these complexes to form supramolecular networks. Different coordinating modes of anions controlled modes of intennolecular interactions, which resulted in different final structures.展开更多
A novel Cu(OAc)_(2)•H_(2)O catalyzed coupling reaction of N-substituted-2-iodobenzamides with malononitrile to afford N-substituted-3-amino-4-cyano-isoquinoline-1(2H)-ones is described.The reaction proceeded in DMSO a...A novel Cu(OAc)_(2)•H_(2)O catalyzed coupling reaction of N-substituted-2-iodobenzamides with malononitrile to afford N-substituted-3-amino-4-cyano-isoquinoline-1(2H)-ones is described.The reaction proceeded in DMSO at 90℃ for 5 h in nitrogen without external ligands.展开更多
文摘The carcinogenic antioxidants,N-phenyl-1-naphthylamine (P1NA)and N-phenyl-2-naphthylamine (P2NA) were examined in vitro for biotransformation by rat hepatic microsomes and in freshly isolated hepatocytes. HPLC-analysis of hepatocyte incubations with revealed that phenols were the major metabolites in both cases. P1NA formed one phenolic metabolite only, while incubation with P2NA yielded two phenols identified as 6-hydroxy-P2NA and 4'-hydroxy-P2NA by cochromatography with authentic samples. β-naphthylamine, a metabolite indicating dephenylation of P2NA was not detectable.Metabolism studies with microsomes revealed that the phenols were formed by cytochrome P-450 dependent monooxygenases. Pretreatment of animals with phenobarbital and 3-methylcholanthrene both increased the rate of microsomal metabolism of P1NA and P2NA, indicating that more than one P-450 enzyme mediate the oxygenation reaction. Animal pretreatment with single and repeated doses of P1NA and P2NA did not markedly stimulate metabolism, but induced ethylmorphine demethylatior. in males and females and benzo (a)pyrene hydroxylation in females.
基金Project supported by the National Natural Science Foundation of China (No. 20132020)
文摘The title compound N-phenyl-2-deoxy-D-ribopyranosylamine featuring a single conformation and pyranose-ring has been synthesized and characterized by NMR spectrum and X-ray diffraction. X-ray crystal structure analysis shows that its crystal belongs to the monoclinic system, space group P21 with a = 6.5375(9), b = 7.7140(9), c = 10.7865(16)A, β= 97.578(11)^o, Z = 2, V= 539.22(13)A^3, Dc = 1.289 g/cm^3, F(000) = 224, μ(MoKa) --- 4.533 mm^-1, R = 0.0305 and wR = 0.0639 for 1093 observed reflections (I 〉 2σ(I). This compound exists as a-conformation and ^1C4 chair-like configuration.
基金Project supported by the National Natural Science Foundation of China (No. 20872033), Hunan Provincial Natural Science Foundation of China (No. 07JJ1003) and Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research (Ministry of Education of China) (No. KLCBTCMR2008-14).
文摘Thirteen novel N-(2-fluoro-5-(3-methyl-2,6-dioxo-4-(trifluoromethy)-2,3-dihydropyrimidin-1(6H)-yl)phenyl)- 2-phenoxy)acetamides were designed and synthesized utilizing 4-fluoro-aniline and ethyl 3-amino-4,4,4-trifluoro-but-2-enoate as starting materials. The chemical structures of all compounds were confirmed by IH NMR, IR, mass spectrum and elemental analyses. Subsequently, the herbicidal activities of the as-prepared compounds were evalu-ated in the greenhouse. Bioassay results indicated that most of compounds had better herbicidal activities against dicotyledonous weeds. Among all the tested compounds, compounds 4a--4i showed good herbicidal activities at both pre-emergence and post-emergence treatment against two or three kinds of dicotyledonous weeds, such as Abutilon theophrasti Medic, Amaranthus ascendens L, and Chenopodium album L at the dosage of 75 g ai/ha.
基金Project supported by the Natural Science Foundation of Education Bureau of Liaoning Province, China.
文摘Three complexes Cu(ppca)2(H2O)2(NO3)2 (1), Cu2(μ-OH)2(ppca)2(H2O)4)·(ClO4)2 (2) and Cu2(μ-CH3COO)4(ppca)2(3) have been synthesized by the reaction of copper(Ⅱ) salts with N-phenyl-4-pyridinecarboxamide (ppca) and characterized. For anions, in complex 1, NO3^- coordinated with copper(Ⅱ), in complex 2 perchlorate anion did not take part in coordination, the copper(Ⅱ) cations were connected by μ-OH to form a dinuclear unit, and complex 3 had a dimeric copper(Ⅱ) carboxylate paddle-wheel core. Noncovalent interactions linked these complexes to form supramolecular networks. Different coordinating modes of anions controlled modes of intennolecular interactions, which resulted in different final structures.
基金We thank the National Natural Science Foundation of China(Nos.20772088 and 21172163)a project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions for funding this work.
文摘A novel Cu(OAc)_(2)•H_(2)O catalyzed coupling reaction of N-substituted-2-iodobenzamides with malononitrile to afford N-substituted-3-amino-4-cyano-isoquinoline-1(2H)-ones is described.The reaction proceeded in DMSO at 90℃ for 5 h in nitrogen without external ligands.