4.5 Article

Synthesis and Vasorelaxant Activity of Nitrate-Coumarin Derivatives

期刊

CHEMMEDCHEM
卷 17, 期 21, 页码 -

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202200476

关键词

Nitrate-coumarins; vasorelaxation; nitroglycerin; sodium nitroprusside; nitric oxide

资金

  1. Xunta de Galicia [ED431B 2020/26, GPC GI-1862]
  2. Ministerio de Ciencia e Innovacion [PID2020-116076RJ-I00/AEI/10.13039/501100011033, PID2020119178GB-I00]
  3. Fundacao para a Ciencia e Tecnologia [PTDC/ASP-PES/28397/2017, CEECIND/02423/2018, UIDB/00081/2020, LA/P/0056/2020, EXPL/BIA-BQM/0492/2021]

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The newly synthesized nitrate-coumarins have been found to possess vasorelaxant activity on rat aorta rings, making them potential alternatives for the development of vasodilator drugs.
Due to the need for new chemical entities for cardiovascular diseases, we have synthesized a new series of nitrate-coumarins and evaluated their vasorelaxant activity in contraction-relaxation studies using rat aorta rings precontracted with phenylephrine or by depolarization with a high concentration of potassium chloride. Four of the new compounds were able to relax smooth vascular muscle with a similar profile and potency to glyceryl trinitrate (IC50=12.73 nM) and sodium nitroprusside (IC50=4.32 nM). Coumarin-7-yl-methyl nitrate (4), the best compound within the series, was able to relax smooth vascular muscle in the low nanomolar range (IC50=1.92 nM). The mechanisms of action have been explored, being the activation of sGC and the opening of K+ channels involved. Our studies indicate that the new nitrate derivatives are reversible and not deleterious for aortic rings, suggesting that these compounds have a potential interest for the development of new and highly efficient vasodilator drugs.

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