The Synthesis Of 4,5-dihydro-[1,2,4]-triazolo [4,3-a] Quinolin Derivatives And The Study Of Its Positive Inotropic Activity

Generally speaking,the mortality caused by angiocardiopathy is declining every year,but the mortality caused by congestive heart failure (CHF) is rising steadily and there is short of effective drugs for CHF in clinic up till the present moment.In order to developing more effective positive inotropic agents having lower side effects,Huri Piao et al reported the synthesis and the positive inotropic activities of 20 4-substitutedpiperazine-1 -acetamido-3,4-dihydroquinolinone derivatives using the principle of isosterism through investigating and analysing the structure and the activities of reported 3,4-dihydroquinolinone derivatives,among which the PHR960012 has been screened and showed the moderate positive inotropic activity followed angiectatic effect and high selectivity (having few effects on the heart rate) in 1999.A series of substituents on the benzene ring of the benzyl group on the PHR960012 which was considered as a lead compound were investigated and the corresponding 14 compounds were synthesized by Huri Piao et al. in2000. The biological tests showed that 8 compounds exhibited stronger activities compared to Milinone and compounds PHR9906 and PHR9903 showed the most significant positive inotropic activities among those compounds.In this paper,a triazole ring being added to the quinoline ring and 19 compounds with different substituents on both rings were synthesized in this paper. Their structures were confirmed by MS,IR,and 1HNMR .