In this work it was presented an application of task specific onium salt as soluble support for the synthesis of 3-amino-5-aryl-2,5- dihydropyridazines. This soluble support is of wide applicability and combines advan...In this work it was presented an application of task specific onium salt as soluble support for the synthesis of 3-amino-5-aryl-2,5- dihydropyridazines. This soluble support is of wide applicability and combines advantages of solid phase synthesis without its limitations with those of solution phase chemistry. After a simple washing step, products were cleaved from the supports and obtained in good yields.展开更多
Many studies have been performed on the pyridazine(1,2-diazine) derivatives in the past decade. This heterocyclic nucleus possesses almost all types of pharmacological activities. This small and simple pyridazine nucl...Many studies have been performed on the pyridazine(1,2-diazine) derivatives in the past decade. This heterocyclic nucleus possesses almost all types of pharmacological activities. This small and simple pyridazine nucleus is present in various compounds that are involved in the research aiming to evaluate new compounds with interesting biological activities, including anti-bacterial, anti-fungal, anti-viral, analgesic, anti-inflammatory, anti-platelets, anti-ulcer, anti-secretory, anti-depressants, anxiolytics, sedative-hypnotics, anti-convulsant, anti-tumor, anti-thrombotics, cardiotonics, vasodilatators, anti-arrhythmics, anti-diabetic, anti-tubercular agents and so on. This review focuses on the pyridazine derivatives with potential activities that have been developed. Pyridazine compounds draw attention of scientists and researchers because of their diverse biological activities as well as simple chemical and easy functionalization at various ring positions, making them attractive synthetic building blocks for designing and development of novel pyridazinone-based therapeutic agents.展开更多
In searching for effective anticonvulsant agents,fourteen 6-aryl-4.5-di- hydro-3(2H)pyridazinones.fifteen 6-aryl-3(2H)pyridazinones,and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized,and evalu...In searching for effective anticonvulsant agents,fourteen 6-aryl-4.5-di- hydro-3(2H)pyridazinones.fifteen 6-aryl-3(2H)pyridazinones,and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized,and evaluated in mice for the ability to antagonize maximal electroshock seizure(MES).The ED_(50) values showed that 6-(2′,4′- dichlorophenyt)-3(2H)pyridazinone was the most potent anticonvulsant among these corn- pounds(ED_(50)=10.15 mg/kg).The structure-activity relationships of the aryl pyridazinones were studied.The result showed that:(1)the higher the value of the hydrophobic parameter л of the substituent on the phenyl ring.the more potent the anticonvulsant activity of the corn- pound.and(2)only the compounds with an electron withdrawing substituent on the phenyl ring exhibited appreciable anticonvulsant activity.展开更多
基金the Natural Sciences Foundation of Hubei province in China(Nos.2007ABA031 and 2008CDA078)
文摘In this work it was presented an application of task specific onium salt as soluble support for the synthesis of 3-amino-5-aryl-2,5- dihydropyridazines. This soluble support is of wide applicability and combines advantages of solid phase synthesis without its limitations with those of solution phase chemistry. After a simple washing step, products were cleaved from the supports and obtained in good yields.
文摘Many studies have been performed on the pyridazine(1,2-diazine) derivatives in the past decade. This heterocyclic nucleus possesses almost all types of pharmacological activities. This small and simple pyridazine nucleus is present in various compounds that are involved in the research aiming to evaluate new compounds with interesting biological activities, including anti-bacterial, anti-fungal, anti-viral, analgesic, anti-inflammatory, anti-platelets, anti-ulcer, anti-secretory, anti-depressants, anxiolytics, sedative-hypnotics, anti-convulsant, anti-tumor, anti-thrombotics, cardiotonics, vasodilatators, anti-arrhythmics, anti-diabetic, anti-tubercular agents and so on. This review focuses on the pyridazine derivatives with potential activities that have been developed. Pyridazine compounds draw attention of scientists and researchers because of their diverse biological activities as well as simple chemical and easy functionalization at various ring positions, making them attractive synthetic building blocks for designing and development of novel pyridazinone-based therapeutic agents.
文摘有关PET心肌血流灌注显像(MPI)无创地检测和评估冠状动脉粥样硬化性心脏病(简称冠心病)的研究正在逐渐增加。但常用的PET MPI显像剂(15O-H2O、13N-NH3·H2O和82Rb)由于其固有的缺点限制了其广泛的临床应用。2-(1,1-二甲基乙基)-4-氯-5{[4-[[2-氟(18F)乙氧基]甲基]苯基]甲氧基}-3-哌啶酮(18F-Flurpiridaz)的研制开创了正电子血流灌注显像剂的新领域。18F-Flurpiridaz的临床前期和临床试验的初步结果显示其具有理想PET MPI显像剂的重要特性,即心肌摄取率高,对图像的灌注缺损判别分辨率高,心肌清除速度慢,随着时间的推移靶/非靶比值稳定,并能定量分析血流,具有较佳的临床应用前景。该文介绍了18F-Flurpiridaz PET MPI的研究现状及进展。
文摘In searching for effective anticonvulsant agents,fourteen 6-aryl-4.5-di- hydro-3(2H)pyridazinones.fifteen 6-aryl-3(2H)pyridazinones,and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized,and evaluated in mice for the ability to antagonize maximal electroshock seizure(MES).The ED_(50) values showed that 6-(2′,4′- dichlorophenyt)-3(2H)pyridazinone was the most potent anticonvulsant among these corn- pounds(ED_(50)=10.15 mg/kg).The structure-activity relationships of the aryl pyridazinones were studied.The result showed that:(1)the higher the value of the hydrophobic parameter л of the substituent on the phenyl ring.the more potent the anticonvulsant activity of the corn- pound.and(2)only the compounds with an electron withdrawing substituent on the phenyl ring exhibited appreciable anticonvulsant activity.
