Citation: Ting Ting Li, Ling Zhang, Zhe Shan Quan, Hai Bo Zhu, Hu Ri Piao. Synthesis and positive inotropic evaluation of 1-(benzylamino)-3-(4,5-di-hydro[1,2,4]trizaolo[4,3-a]quinolin-7-yloxy)propan-2-ol derivatives[J]. Chinese Chemical Letters, ;2009, 20(2): 175-177. doi: 10.1016/j.cclet.2008.11.003 shu

Synthesis and positive inotropic evaluation of 1-(benzylamino)-3-(4,5-di-hydro[1,2,4]trizaolo[4,3-a]quinolin-7-yloxy)propan-2-ol derivatives

a Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, China;
b Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China

Received Date: 28 August 2008

Fund Project: This work was supported by the National Natural Science Foundation of China (No. 30560177) and the Natural Science Foundation of Jilin Province of China (No. 20060567).

In an attempt to search for more potent positive inotropic agents, a series of 1-(benzylamino)-3-(4,5-dihydro[1,2,4]trizaolo[4,3-a]quinolin-7-yloxy)propan-2-ol derivatives was synthesized in four steps using 6-hydroxy-3,4-dihydro-2(1H)-quinolinone as a starting material, and their positive inotropic activities were evaluated by measuring the coronary blood flow (CBF) and the left ventricular pressure (LVP) followed by calculating the rate of pressure development (dp/dt_max values) in the preparation of rat Langendorff's heart. Three compounds (5d, 5g, 5j) showed favorable activities, among which 5g was shown the most potent with dp/dt_max value of 9.7% and CBF value of 17.8% at a concentration of 1×10^-5 mol/L in our in vitro study.
- 3,4-Dihydro[1,
- 2,
- 4]trizaolo[4,
- 3-a]quinoline,
- Positive inotropic activity,
- Synthesis
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