The gasotransmitter hydrogen sulfide (H₂S) is an important tuner of the cardiovascular homeostasis, and its deficiency is etiologically associated with a number of cardiovascular diseases. Therefore, the research of original moieties able to release H₂S represents a timely issue for drug discovery. In this work, we developed a collection of iminothioethers (ITEs), exhibiting H₂S-releasing properties and producing vasorelaxing effects on rat aortic rings. Derivatives 4 and 11, selected as representative of slow and fast rate H₂S donors, respectively, produced a complete recovery of the basal coronary flow, reverting the AngII-induced effects in isolated rat hearts. In addition, studies on human aortic smooth muscle cells (HASMCs) demonstrated membrane hyperpolarizing effects, well related to the intracellular generation of H₂S. Taken together, the results obtained support ITEs 4 and 11 as new pharmacological tools, as well as effective and innovative H₂S donors for cardiovascular drug discovery.

中文翻译：

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亚氨基硫醚作为硫化氢的供体：从气体递质释放到血管效应

气体递质硫化氢（H ₂ S）是心血管稳态的重要调节剂，其缺乏在病因上与许多心血管疾病有关。因此，对能够释放H ₂ S的原始部分的研究代表了药物发现的及时问题。在这项工作中，我们开发了亚氨基硫醚（ITE）的集合，这些亚硫醚具有H ₂ S释放特性，并且对大鼠主动脉环产生血管松弛作用。选择导数4和11作为慢速和快速H _2的代表S个供体分别使基础冠状动脉血流完全恢复，从而恢复了AngII诱导的离体大鼠心脏的作用。此外，对人主动脉平滑肌细胞（HASMC）的研究表明，膜超极化作用与H ₂ S的细胞内生成密切相关。综上所述，所获得的结果支持ITE 4和ITE 11作为新的药理学手段，并且有效且有效。用于心血管药物发现的创新型H ₂ S供体。