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1.
Org Lett ; 26(6): 1249-1254, 2024 Feb 16.
Artigo em Inglês | MEDLINE | ID: mdl-38305700

RESUMO

An efficient copper catalytic system has been established for the synthesis of highly functional indolizines through oxidative [3 + 2] cycloaddition of enamines and pyridotriazoles. This modular platform is compatible with a broad range of functional groups, including natural and complex skeletons, allowing for late-stage modifications. It features a step-economical, highly regioselective, and easy-handling procedure and has been applied in constructing small molecules of potent activity toward inhibiting the VEGF-NRP1 interaction through a one-pot reaction of pyridotriazoles, amines, and aldehydes.

2.
Chem Commun (Camb) ; 58(21): 3525-3528, 2022 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-35195654

RESUMO

This study describes a cascade method for the synthesis of ß-aminoketones through the reductive hydroamination of alkynes under very mild metal-free conditions. It allows for the rapid conversion of ynones and amines into corresponding ß-aminoketones with a broad substrate scope and diverse functionalities. This straightforward and easy-to-handle reaction process can be successfully applied for the synthesis of Proroxan and Propipocaine, offering a potential option for the synthesis of drug molecules with the ß-aminoketone skeleton.

3.
Asian Pac J Trop Med ; 9(8): 791-5, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27569890

RESUMO

OBJECTIVE: To investigate the effects of exogenous recombinant human brain natriuretic peptide (rhBNP) after primary percutaneous coronary intervention (PCI) on non-invasive hemodynamic in acute myocardial infarction patients with left ventricular failure. METHODS: A number of 96 acute myocardial infarction patients accompanied with heart failure after PCI hospitalized in the People's Hospital of Sanya during February 2012 to October 2015 were selected. They were randomly divided into the therapy group (n = 50) and control group (n = 46). On the basis of routine treatment, patients in the therapy group were treated with intravenous rhBNP (1.5 µg/kg was intravenous injection with uniform speed of 3 min, followed by continuous infusion 0.0075 µg/kg·min for 72 h), while the control group received conventional treatment. BioZ-2011 non-invasive hemodynamic real-time monitoring system was used to monitor the hemodynamic parameters changes and the leaves of plasma pro-BNP, serum creatinine, serum potassium, serum sodium and urine volume of each group before and after treating for 30 min, 1 h, 3 h, 6 h, 12 h, 24 h, 48 h, 72 h. RESULTS: Patients in the therapy group showed no effect on heart rate, while after 30 min of intravenous injection of rhBNP, CO, CI, SV, and SI increased significantly and LVET and TFC reduced at the same time, which had certain effect on blood pressure (SBP/DBP). Compared with the control group, the therapy group showed a faster and more effective improvement on hemodynamics. CONCLUSIONS: Acute myocardial infarction patients complicated with left heart failure after primary PCI can significantly improve hemodynamics by treating with rhBNP.

4.
Asian Pac J Trop Med ; 9(2): 172-6, 2016 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-26919950

RESUMO

OBJECTIVE: To investigate the correlation between E670G polymorphism of proprotein convertase subtilisin/kexin type 9 (PCSK9) gene and coronary heart disease (CHD), and contrastively study the regional differences of E670G polymorphism of PCSK9 gene between patients with CHD among the Han population in Hainan and three provinces in the northeast of China (TPNC), providing scientific basis for prevention and treatment of patients with CHD in different regions. METHODS: A total of 233 cases of patients with CHD were selected from the Han population in Hainan and TPNC as the experimental group (118 cases from Hainan, 115 cases from TPNC), and 239 cases with non-CHD were selected among the Han population also in the two regions as control group (125 cases from Hainan, 114 cases from TPNC). The triglyceride (TG), total cholesterol (TC), high density lipoprotein cholesterol and low density lipoprotein cholesterol (LDL-C) levels of plasma were tested and PCR-RFLP method was used to test the E670G polymorphism of PCSK9 gene. The statistical software package SPSS 21.0 was used for the statistical analysis and P < 0.05 was considered as statistically significant. RESULTS: The levels of systolic pressure, diastolic blood pressure, fasting blood sugar, TC, TG, and LDL-C of patients in CHD group were significantly higher than those in non-CHD group, while the high density lipoprotein cholesterol level was lower than that in non-CHD group (P < 0.05). In CHD group, the frequencies of AG, GG genotypes of PCSK9 gene and G allele were higher than those in non-CHD group (P < 0.05), and in CHD group, the frequencies of AG, GG genotypes and G allele of patients both in Hainan and TPNC were higher than those in control group (P < 0.05). Among the patients with CHD, the frequencies of GG genotype and G allele of patients in Hainan were lower than those in TPNC (P < 0.05), and in CHD group, the levels of TG, TC and LDL-C of GG genotype were higher than those of AA genotype (P < 0.05). While in non-CHD group, there were no significant differences between the frequencies of GG genotype and G allele of patients in Hainan and TPNC (P > 0.05). CONCLUSIONS: There was a close correlation between the E670G polymorphism of PCSK9 gene and CHD with serum lipid level. Among Han population in Hainan and TPNC, the E670G polymorphism of PCSK9 gene of patients with CHD exhibited regional differences.

5.
Nan Fang Yi Ke Da Xue Xue Bao ; 31(7): 1277-8, 2011 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-21764714

RESUMO

OBJECTIVE: To explore the correlation between serum levels of growth differentiation factor-15 (GDF-15) and Thrombolysis in Myocardial Infarction (TIMI) risk scores in patients with unstable angina pectoris (UA). METHODS: The serum levels of GDF-15 in 97 patients with UA and 30 healthy volunteers were measured using enzyme-linked immunosorbent assay (ELISA) and compared between 3 patient groups with different TIMI scores to analyze relationship between serum GDF-15 levels and TIMI risk scores. RESULTS: The serum levels of GDF-15 in UA patients were significantly higher than those in the healthy volunteers (P<0.01). GDF-15 levels also differed significantly between patients with different TIMI scores (P<0.01), and showed a significant positive correlation to TIMI risk scores. CONCLUSION: Serum levels of GDF-15 can be used as an index for evaluating the severity of UA.


Assuntos
Angina Instável/sangue , Fator 15 de Diferenciação de Crescimento/sangue , Terapia Trombolítica/efeitos adversos , Idoso , Angina Instável/tratamento farmacológico , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Medição de Risco , Índice de Gravidade de Doença
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