引用本文:
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
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
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
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
摘要:
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/dtmax 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.
-
关键词:
- 3,4-Dihydro[1
- / 2
- / 4]trizaolo[4
- / 3-a]quinoline
- / Positive inotropic activity
- / Synthesis
English
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
Abstract:
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/dtmax 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.
-
Key words:
- 3,4-Dihydro[1
- / 2
- / 4]trizaolo[4
- / 3-a]quinoline
- / Positive inotropic activity
- / Synthesis
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