Wang Teng, Dong Ying, Wang Li-Chen, Xiang Bing-Ren, Chen Zhen, Qu Ling-Bo
Center for Instrumental Analysis, China Pharmaceutical University, Nanjing, The People's Republic of China.
Arzneimittelforschung. 2008;58(11):569-73. doi: 10.1055/s-0031-1296558.
Based on our previous study, a variety of 12 novel 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives were synthesized. The structures attributed to the compounds were elucidated using IR, 1H-NMR and mass spectra. The cardiotonic activities of these compounds were assessed by Straub's perfusion method and a clear cardiotonic effect was shown for compounds 1c (2,3-dichloro-N-(4-(4-methyl-6-oxo-1,4,5,6-tetrahydro-pyridazin-3-yl)phenyl) benzamide), 1d (4-amino-3-methyl-N-(4-(4-methyl-6-oxo-1,4,5,6-tetrahydropyridazin-3-yl) phenyl)benzamide), 2a (3-methyl-4-nitro-N-(4-(6-oxo-1,4,5,6-tetrahydro-pyridazin-3-yl)phenyl)benzamide) and 2d (4-amino-3-methyl -N-(4-(6-oxo-1,4,5,6-tetrahydropyridazin-3-yl)phenyl) benzamide) when compared to another 3(2H)-pyridazinone derivative, levosimendan (CAS 141505-33-1). The structure-activity relationships of the compounds were studied using the rough sets theory.
基于我们之前的研究，合成了12种新型的6-苯基-4,5-二氢-3(2H)-哒嗪酮衍生物。通过红外光谱(IR)、氢核磁共振波谱(1H-NMR)和质谱对这些化合物的结构进行了鉴定。采用施特劳布灌注法评估了这些化合物的强心活性，与另一种3(2H)-哒嗪酮衍生物左西孟旦（化学物质登记号141505-33-1）相比，化合物1c（2,3-二氯-N-(4-(4-甲基-6-氧代-1,4,5,6-四氢哒嗪-3-基)苯基)苯甲酰胺）、1d（4-氨基-3-甲基-N-(4-(4-甲基-6-氧代-1,4,5,6-四氢哒嗪-3-基)苯基)苯甲酰胺）、2a（3-甲基-4-硝基-N-(4-(6-氧代-1,4,5,6-四氢哒嗪-3-基)苯基)苯甲酰胺）和2d（4-氨基-3-甲基-N-(4-(6-氧代-1,4,5,6-四氢哒嗪-3-基)苯基)苯甲酰胺）显示出明显的强心作用。利用粗糙集理论研究了这些化合物的构效关系。
