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Synthesis and Vasorelaxant Activity of Nitrate−Coumarin Derivatives
dc.contributor.author | Matos, Maria João | |
dc.contributor.author | Uriarte, Eugenio | |
dc.contributor.author | Seoane, Nuria | |
dc.contributor.author | Picos, Aitor | |
dc.contributor.author | Gil-Longo, José | |
dc.contributor.author | Campos-Toimil, Manuel | |
dc.date.accessioned | 2024-04-10T06:21:31Z | |
dc.date.available | 2024-04-10T06:21:31Z | |
dc.date.issued | 2022 | |
dc.identifier.issn | 18607179 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12728/10968 | |
dc.description.abstract | 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. © 2022 The Authors. ChemMedChem published by Wiley-VCH GmbH. | es_ES |
dc.description.sponsorship | Xunta de Galicia: Plan Galego IDT, (ED431B 2020/26, GPC GI‐1862); Fundação para a Ciência e a Tecnologia, FCT, (CEECIND/02423/2018, EXPL/BIA‐BQM/0492/2021, LA/P/0056/2020, PTDC/ASP‐PES/28397/2017, UIDB/00081/2020); Ministerio de Ciencia e Innovación, MICINN, (PID2020‐116076RJ‐I00/AEI/10.13039/501100011033, PID2020‐119178GB‐I00) | es_ES |
dc.language.iso | en | es_ES |
dc.publisher | John Wiley and Sons Ltd | es_ES |
dc.subject | Nitrate−coumarins | es_ES |
dc.subject | nitric oxide | es_ES |
dc.subject | nitroglycerin | es_ES |
dc.subject | sodium nitroprusside | es_ES |
dc.subject | vasorelaxation | es_ES |
dc.title | Synthesis and Vasorelaxant Activity of Nitrate−Coumarin Derivatives | es_ES |
dc.type | Article | es_ES |