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 |
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| Authors: | Ting Ting Lia Ling Zhangb Zhe Shan Quana Hai Bo Zhu Hu Ri Piao a Key Laboratory of Natural Resources Functional Molecules of the Changbai Mountain Affiliated Ministry of Education Yanbian University College of Pharmacy Yanji China b lnstitate of Materia Medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing China |
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| Institution: | 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 |
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| Abstract: | In an attempt to search for more potent positive inotropic agents,a series of 1-(benzylamino)-3-(4,5-dihydro1,2,4]trizaolo4,3-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/dtmx 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/dtmax value of 9.7% and CBF value of 17.8% at a concentration of 1×10-5 mol/L in our in vitro study. |
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| Keywords: | 3 4-Dihydro[1 2 4]trizaolo[4 3-a]quinoline Positive inotropic activity Synthesis |
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