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Cited by 179

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Arylthioamides as H2S Donors: l-Cysteine-Activated Releasing Properties and Vascular Effects in Vitro and in Vivo

Open access
Martelli, Alma, Testai, Lara, Citi, Valentina, Marino, Alice, Pugliesi, Isabella, Barresi, Elisabetta, Nesi, Giulia, Rapposelli, Simona, Taliani, Sabrina, Da Settimo, Federico, Breschi, Maria C., Calderone, Vincenzo·2013·ACS Medicinal Chemistry Letters

Abstract

A small library of arylthioamides 1-12 was easily synthesized, and their H2S-releasing properties were evaluated both in the absence or in the presence of an organic thiol such as l-cysteine. A number of arylthioamides (1-3 and 7) showed a slow and l-cysteine-dependent H2S-releasing mechanism, similar to that exhibited by the reference slow H2S-releasing agents, such as diallyl disulfide (DADS) and the phosphinodithioate derivative GYY 4137. Compound 1 strongly abolished the noradrenaline-induced vasoconstriction in isolated rat aortic rings and hyperpolarized the membranes of human vascular smooth muscle cells in a concentration-dependent fashion. Finally, a significant reduction of the systolic blood pressure of anesthetized normotensive rats was observed after its oral administration. Altogether these results highlighted the potential of arylthioamides 1-3 and 7 as H2S-donors for basic studies, and for the rational design/development of promising pharmacotherapeutic agents to treat cardiovascular diseases.

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Metadata

Authors
Martelli, A., Testai, L., Citi, V., Marino, A., Pugliesi, I., Barresi, E., Nesi, G., Rapposelli, S., Taliani, S., Da Settimo, F., Breschi, M. C., & Calderone, V.
Venue
ACS Medicinal Chemistry Letters
Published
2013-08-12
Volume
4
Issue
10
Pages
904-908
ISSN
1948-5875 (ISSN-L)
OpenAlex
W1973549188
Cited by
179
References
1
FWCI
3.62
Type
journal article
Language
en
Open access
green

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CoChat. (2026). Citation check: Arylthioamides as H2S Donors: l-Cysteine-Activated Releasing Properties and Vascular Effects in Vitro and in Vivo. https://app.cochat.ai/papers/10.1021/ml400239a
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Martelli, A., Testai, L., Citi, V., Marino, A., Pugliesi, I., Barresi, E., Nesi, G., Rapposelli, S., Taliani, S., Da Settimo, F., Breschi, M. C., & Calderone, V. (2013). Arylthioamides as H2S Donors: l-Cysteine-Activated Releasing Properties and Vascular Effects in Vitro and in Vivo. ACS Medicinal Chemistry Letters. https://doi.org/10.1021/ml400239a

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