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Evaluation of thioamides, thiolactams and thioureas as hydrogen sulfide (H2S) donors for lowering blood pressure.

Abstract：

:Hydrogen sulfide (H2S) is a biologically important gaseous molecule that exhibits promising protective effects against a variety of pathological processes. For example, it was recognized as a blood pressure lowering agent. Aligned with the need for easily modifiable platforms for the H2S supply, we report here the preparation and the H2S release kinetics from a series of structurally diversified thioamides, thiolactams and thioureas. Three different thionation methods based on the usage of a phosphorus pentasulfide and Lawesson reagent were applied to prepare the target thioamides and thiolactams. Furthermore, obtained H2S donors were evaluated both in in vivo and in vitro studies. The kinetic parameters of the liberating H2S was determined and compared with NaHS and GYY4137 using two different detection technics i.e.; fluorescence labeling 7-azido-4-methyl-2H-chromen-2-one and 5,5'-dithiobis (2-nitrobenzoic acid), sulfhydryl probe, also known as the Ellman's reagent. We have proved that the amount of releasing H2S from these compounds is controllable through structural modifications. Finally, the present study shows a hypotensive response to an intravenous administration of the developed donors in the anesthetized rats.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Zaorska E,Hutsch T,Gawryś-Kopczyńska M,Ostaszewski R,Ufnal M,Koszelewski D

doi

10.1016/j.bioorg.2019.102941

subject

Has Abstract

pub_date

2019-07-01 00:00:00

pages

102941

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)30252-4

journal_volume

88

pub_type

杂志文章

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