作者机构：
[Liu, ZJ] Cent China Normal Univ, Inst Organ Synth, Wuhan 430079, Peoples R China.;NanHua Univ, Coll Chem & Chem Engineer, Hengyang 421001, Peoples R China.
通讯机构：
[Liu, ZJ] C;Cent China Normal Univ, Inst Organ Synth, Wuhan 430079, Peoples R China.
摘要：
Reaction of 3-methylthio-1-phenyl-5-{[( triphenyl-lambda(5)-phosphanylidene)methane] -amino}-1H-pyrazole-4-carboxylic acid ethyl ester with ROH in the presence of RONa or passium. carbonate affords 6-alkoxyl/aroxyl-3-alkylthio-1,5-diphenyl-1,5-dihydropyrazolo[3,4-d]pyrimidin -4-one.
摘要：
Type 2 diabetes is a major risk factor of the development of atherosclerosis in humans. However, studies examining mechanisms underlying diabetes-accelerated atherosclerosis have been limited by the lack of suitable humanoid animal models. Pigs have a cardiovascular system that is very similar to that of humans and is useful as a model for human physiology and pathophysiology. In this study, we established a new miniature pig model for studying dyslipidaemia and atherosclerosis in diabetes. Chinese Guizhou minipigs were fed a normal control diet or a high-fat/high-sucrose diet (HFSD) for 6 months. Plasma total cholesterol (TC), high-density lipoprotein cholesterol, triglyceride (TG), insulin and glucose were quantified at monthly intervals. The induction of insulin resistance and dysfunction of the pancreatic β-cell were assessed by oral glucose tolerance test and insulin sensitivity test. The aortic fatty streak lesions were quantified following lipid staining with Sudan IV. During the feeding period, mild high plasma TC and TG were induced. At the end of 6 months, in HFSD-fed animals, the adipocytes were hypertrophic, fat deposit in the liver was observed, loss of pancreatic β-cells was observed, and the aortic fatty streak lesions were clearly present in the animals' aortas. Our study established that miniature pigs that were fed a HFSD without adding dietary cholesterol developed insulin resistance, mild diabetes and atherosclerotic lesions. HFSD-fed miniature pigs may be good animal models for research on the treatment of diabetic dyslipidaemia complicated with atherosclerosis.
摘要：
A series of new 6-alkylamino-3-alkylthio-1-phenyl-1H-pyrazolo[3,4-d] pyrimidin-4(5H)-one derivatives 5 and 6 have been rapidly synthesized by a novel solution-phase regioselective synthetic method. Treatment of pyrazole o-aminoester 1 with dibromotriphenylphosphorane gave iminophosphorane 2, which underwent a aza-Wittig reaction with phenyl ioscyanate to provide the carbodiimide 3. The latter intermediate reacted with alkylamines and regioselectively provided the 1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-one derivatives 5 and 6, some of which exhibited good fungicidal activity.
作者机构：
[Yin, WD] Department of Biochemistry and Molecular Biology, Nanhua University School of Life Sciences and Technology, Hengyang, 421001, Hunan, China. wdy20012001@yahoo.com
摘要：
The synthetic compound NO-1886 is a lipoprotein lipase activator that has been proven to be highly effective in lowering plasma triglycerides and elevating high-density lipoprotein cholesterol. Recently, we found that NO-1886 also had a plasma glucose-reducing action in high-fat/high-sucrose diet-induced diabetic rabbits. In the current study we investigated the effects of NO-1886 on the morphology of adipocytes, plasma levels of tumor necrosis factor-alpha (TNF-alpha) and free fatty acids (FFA) in miniature pigs fed a high-fat/high-sucrose diet. Our results showed that feeding a high-fat/high-sucrose diet to miniature pigs increased the size of adipocytes, and the plasma levels of TNF-alpha, FFA, and glucose. This diet also induced insulin resistance and impaired the acute insulin response to glucose loading. Supplementing 1% NO-1886 to the high-fat/high-sucrose diet inhibited adipocyte enlargement, and suppressed plasma levels of TNF-alpha, FFA, and glucose. The decrease in plasma TNF-alpha and FFA was simultaneous with the decrease in plasma glucose. We also found an increased whole body glucose clearance and an increased acute insulin response to intravenous glucose loading by NO-1886 supplementation. These data suggest that NO-1886 improves the glucose metabolism in high-fat/high-sucrose diet-induced diabetic minipigs by decreasing fat deposit, and suppressing plasma TNF-alpha and FFA levels. Therefore, NO-1886 is potentially beneficial for the treatment of insulin-resistant syndrome. (C) 2003 Elsevier Ltd. All rights reserved.
期刊：
Journal of Heterocyclic Chemistry,2004年41(3):393-397 ISSN：0022-152X
通讯作者：
Liu, ZJ
作者机构：
[Liu, ZJ] Cent China Normal Univ, Inst Organ Synth, Wuhan 430079, Peoples R China.;NanHua Univ, Coll Chem & Chem Engineer, Hengyang 421001, Peoples R China.
通讯机构：
[Liu, ZJ] C;Cent China Normal Univ, Inst Organ Synth, Wuhan 430079, Peoples R China.
摘要：
A series of new 1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one Derivatives 5 has been designed and regio-selectively synthesized via a tandem aza-Wittig reaction. The structures of all compounds prepared have been confirmed by 1H NMR, IR, EI-MS spectroscopy and elemental analyses. The results of preliminary bioassay indicate that most compounds 5 possess an inhibition effect against Botrytis cinereapers and Pyricularia oryzae at the concentration of 50 mg/L.
摘要：
The title compound (C25H20FN5OS) has been synthesized and its crystal structure was determined by X-ray analysis. The crystal belongs to the orthorhombic system, space group Pbca with a = 10.327(4), b = 20.307(7), c = 21.234(9)(A), α = 90, β = 90, γ = 90°, V = 4453(3) (A)3, Z = 8, Dc = 1.365 g/cm3, Mr = 457.52, μ = 0.182 mm-1, F(000) = 1904, the final R = 0.0600 and wR = 0.0932 for 3911obsered reflections with I≥2σ(I). In the title compound, the S(1), C(1), C(2), C(3), C(4), C(5), N(1), N(2), N(3), N(4), O(1) and N(5) atoms form a mean planeⅠroughly within the average deviation of 0.0207 (A). The dihedral angles between planesⅠandⅡ(C(19)-C(20)- C(21)-C(22)-C(23)-C(24)),Ⅲ(C(6)-C(7)-C(8)-C(9)-C(10)-C(11)) and Ⅳ(C(12)-C(13)-C(14)- C(15)-C(16)-C(17)-C(18)-F(1)) are 21.40, 84.00 and 75.88o, respectively.
期刊：
Energy & Fuels,2003年17(2):344-347 ISSN：0887-0624
通讯作者：
Wang, YF
作者机构：
[Wang, YF] Cent S Inst Technol, Dept Chem Engn, Hengyang 421001, Hunan, Peoples R China.;Petr Univ China, Natl Lab Heavy Oil Proc, Shandong 257062, Peoples R China.;E China Univ Sci & Technol, Shanghai 200237, Peoples R China.
通讯机构：
[Wang, YF] C;Cent S Inst Technol, Dept Chem Engn, Hengyang 421001, Hunan, Peoples R China.
摘要：
VR (vacuum residua) and CCB oil (catalytic cracking bottom oil) are complex mixtures of hydrocarbons. The investigation of the compatibility and the incompatibility of them is helpful to optimize the ratio of CCB oil/VR in FCC processing and VR solvent deasphalting processing to prevent troubles. In the present work, the mixture property of VR with CCB oil was studied from the standpoint of colloidal dispersion in several different experiments. The investigation shows that in the course of CCB oil being blended with VR, there are two competitive processes of dissolution and flocculation, and the CCB oil's function is to act as both solvent and dispersant. At a low blending ratio of CCB oil, flocculation is almost balanced with dissolution; VR is almost compatible with CCB oil. When the blending ratio of CCB oil is increased, the solvation and dispersal powers of the CCB oil break through the tolerance limit of VR colloidal system, and flocculation predominates over dissolution, which leads to phase separation in the colloidal system and to deposition of the asphaltenes. Under this condition, VR is incompatible with CCB oil.
摘要：
Lipoprotein lipase (LPL) is a rate-limiting enzyme that hydrolyzes circulating triglyceride-rich lipoproteins such as very low-density lipoproteins and chylomicrons. A decrease in LPL activity is associated with an increase in plasma triglycerides (TG) and a decrease in plasma high-density lipoprotein cholesterol (HDL-C). The increase in plasma TG and decrease in plasma HDL-C are risk factors for cardiovascular disease. Tsutsumi et al. hypothesized that elevating LPL activity would cause a reduction of plasma TG and an increase in plasma HDL-C, resulting in protection against the development of atherosclerosis. To test this hypothesis, Otsuka Pharmaceutical Factory, Inc. synthesized the LPL activator NO-1886. NO-1886 increased LPL mRNA and LPL activity in adipose tissue, myocardium and skeletal muscle, resulting in an elevation of postheparin plasma LPL activity and LPL mass in rats. NO-1886 also decreased plasma TG concentration and caused a concomitant rise in plasma HDL-C. Long-term administration of NO-1886 to rats and rabbits with experimental atherosclerosis inhibited the development of atherosclerotic lesions in coronary arteries and aortas. Multiple regression analysis suggested that the increase in plasma HDL-C and the decrease in plasma TG protect from atherosclerosis. The atherogenic lipid profile is changed to an antiatherogenic profile by increasing LPL activity, resulting in protection from of atherosclerosis. Therefore, the LPL activator NO-1886 or other possible LPL activating agents are potentially beneficial for the treatment of hypertriglyceridemia, hypo-HDL cholesterolemia, and protection from atherosclerosis.
