潜在钙通道调节剂环五吡啶和噻吩吡啶衍生物的合成。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-04-01 Epub Date: 2012-01-27 DOI:10.1055/s-0031-1299744
M G Gündüz, C Safak, B Kaygısız, B C Koşar, R Simşek, K Erol, A Linden
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引用次数: 1

摘要

本研究通过改进的Hantzsch反应合成了含环戊酮(1-21)或四氢噻吩-1,1-二氧化环(22-42)的新型缩合1,4-二氢吡啶,并在离体大鼠回肠和胸主动脉上研究了它们的钙通道调节活性。在1,4-二氢吡啶核上引入环戊酮环,在酯基上引入甲基、乙基和烯丙基,使得钙调节剂活性更高。
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Synthesis of cyclopentapyridine and thienopyridine derivatives as potential calcium channel modulators.

In this study, novel condensed 1,4-dihydropyridines bearing cyclopentanone (1-21) or tetrahydrothiophene-1,1-dioxide ring (22-42) with various ester substituents were synthesized via a modified Hantzsch reaction and their calcium channel modulator activities were investigated on isolated rat ileum and rat thoracic aorta. The introduction of a cyclopentanone ring fused to the 1,4-dihydropyridine nucleus and methyl, ethyl and allyl moieties to the ester group led to more active calcium modulators.

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