Hydrogen sulfide (H2S) is an endogenous modulator that plays significant physio-pathological roles in several biological systems. In this research field there is a large interest in developing selective CBS and CSE inhibitors and H2S releasing moieties, that could be either used as therapeutic agents or linked to known drugs. One of the major problem is the limited availability of chemicals that ensure a controlled release of H2S in vitro as well in vivo. Aiming to obtain novel H2S donors, whose release properties could be appropriately modulated, we have synthesized a series of 1,2,4-thiadiazolidine-3,5-diones (THIA 1 e10) as innovative donors that could release H2S in controlled manner. All the synthesized compounds were evaluated for their H2S releasing properties by an amperometric approach and for their vasorelaxant ability on aorta rings. In order to rationalize the obtained results, a detailed study on the release mechanism has been performed using the most efficient H2S donor, THIA 3 (Cmax 65.4 mM and EC50 1.7 mM).

1,2,4-Thiadiazolidin-3,5-diones as novel hydrogen sulfide donors / Severino, Beatrice; Corvino, Angela; Fiorino, Ferdinando; Luciano, Paolo; Frecentese, Francesco; Magli, Elisa; Saccone, Irene; Di Vaio, Paola; Citi, Valentina; Calderone, Vincenzo; Servillo, Luigi; Casale, Rosario; Cirino, Giuseppe; Vellecco, Valentina; Bucci, Mariarosaria; Perissutti, Elisa; Santagada, Vincenzo; Caliendo, Giuseppe. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 143:(2018), pp. 1677-1686. [10.1016/j.ejmech.2017.10.068]

1,2,4-Thiadiazolidin-3,5-diones as novel hydrogen sulfide donors

Severino, Beatrice
;
Corvino, Angela;Fiorino, Ferdinando;Luciano, Paolo;Frecentese, Francesco;Magli, Elisa;Saccone, Irene;Di Vaio, Paola;Cirino, Giuseppe;Vellecco, Valentina;Bucci, Mariarosaria;Perissutti, Elisa;Santagada, Vincenzo;Caliendo, Giuseppe
2018

Abstract

Hydrogen sulfide (H2S) is an endogenous modulator that plays significant physio-pathological roles in several biological systems. In this research field there is a large interest in developing selective CBS and CSE inhibitors and H2S releasing moieties, that could be either used as therapeutic agents or linked to known drugs. One of the major problem is the limited availability of chemicals that ensure a controlled release of H2S in vitro as well in vivo. Aiming to obtain novel H2S donors, whose release properties could be appropriately modulated, we have synthesized a series of 1,2,4-thiadiazolidine-3,5-diones (THIA 1 e10) as innovative donors that could release H2S in controlled manner. All the synthesized compounds were evaluated for their H2S releasing properties by an amperometric approach and for their vasorelaxant ability on aorta rings. In order to rationalize the obtained results, a detailed study on the release mechanism has been performed using the most efficient H2S donor, THIA 3 (Cmax 65.4 mM and EC50 1.7 mM).
2018
1,2,4-Thiadiazolidin-3,5-diones as novel hydrogen sulfide donors / Severino, Beatrice; Corvino, Angela; Fiorino, Ferdinando; Luciano, Paolo; Frecentese, Francesco; Magli, Elisa; Saccone, Irene; Di Vaio, Paola; Citi, Valentina; Calderone, Vincenzo; Servillo, Luigi; Casale, Rosario; Cirino, Giuseppe; Vellecco, Valentina; Bucci, Mariarosaria; Perissutti, Elisa; Santagada, Vincenzo; Caliendo, Giuseppe. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 143:(2018), pp. 1677-1686. [10.1016/j.ejmech.2017.10.068]
File in questo prodotto:
File Dimensione Formato  
EJMC, 2018, 143, 1677-1686.pdf

solo utenti autorizzati

Tipologia: Versione Editoriale (PDF)
Licenza: Copyright dell'editore
Dimensione 1.39 MB
Formato Adobe PDF
1.39 MB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/697753
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 39
  • ???jsp.display-item.citation.isi??? 36
social impact