| Literature DB >> 28799763 |
Elisabetta Barresi1, Giulia Nesi1, Valentina Citi1, Eugenia Piragine1, Ilaria Piano1, Sabrina Taliani1, Federico Da Settimo1, Simona Rapposelli1, Lara Testai1, Maria Cristina Breschi1, Claudia Gargini1, Vincenzo Calderone1, Alma Martelli1.
Abstract
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.Entities:
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Year: 2017 PMID： 28799763 DOI： 10.1021/acs.jmedchem.7b00888
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446