Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2021-01-12 , DOI: 10.1016/j.bmcl.2021.127785 Chang-Bo Zheng 1 , Wen-Cong Gao 1 , Pan-Pan Pang 1 , Xin Ma 1 , Li-Chun Peng 1 , Liang Yang 2 , Xun Li 3
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An array of novel 7-methoxyl-2,3-disubstituted quinoxaline derivatives was designed, synthesized and their potential antihypertensive activities were examined, in an attempt to discover potent small molecules with vasorelaxant effects. The vasoactivities of these compounds on vascular tone, as well as underlying mechanisms were hereby explored. Results showed that five compounds (7s, 7t, 7v, 7w, 7γ) could induce endothelium-independent relaxation in high extracellular K+- and phenylephrine-precontracted C57 mice aortic rings. These five compounds, unlike other commonly used vasodilators, could slowly but effectively inhibit vasoconstriction.
中文翻译：
新型 7-甲氧基-2,3-二取代-喹喔啉衍生物的合成和血管舒张评价
设计、合成了一系列新型 7-甲氧基-2,3-二取代喹喔啉衍生物并检查了它们的潜在抗高血压活性，试图发现具有血管舒张作用的有效小分子。在此探讨了这些化合物对血管张力的血管活性以及潜在机制。结果表明，5 种化合物（7s、7t、7v、7w、7γ）可以诱导高细胞外 K + - 和去氧肾上腺素预收缩 C57 小鼠主动脉环的内皮非依赖性舒张。与其他常用的血管扩张剂不同，这五种化合物可以缓慢但有效地抑制血管收缩。
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