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Bifunctional Sildenafil Diazeniumdiolates Acting as Phosphodiesterase 5 Inhibitors and Nitric Oxide Donors- Towards Wound Healing.
Mas-Roselló, Josep; Tenor, Hermann; Szabo, Timea; Naef, Reto; Sieber, Simon; Gademann, Karl.
Afiliación
  • Mas-Roselló J; Department of Chemistry, University of Zurich, 8057, Zurich, Switzerland.
  • Tenor H; Topadur Pharma AG, Grabenstrasse 11A, 8952, Schlieren, Switzerland.
  • Szabo T; Department of Chemistry, University of Zurich, 8057, Zurich, Switzerland.
  • Naef R; Topadur Pharma AG, Grabenstrasse 11A, 8952, Schlieren, Switzerland.
  • Sieber S; Department of Chemistry, University of Zurich, 8057, Zurich, Switzerland.
  • Gademann K; Department of Chemistry, University of Zurich, 8057, Zurich, Switzerland.
Chembiochem ; 25(8): e202300801, 2024 Apr 16.
Article en En | MEDLINE | ID: mdl-38430555
ABSTRACT
Inefficient wound healing poses a global health challenge with a lack of efficient treatments. Wound healing issues often correlate with low endogenous nitric oxide (NO) levels. While exogenous delivery with NO-releasing compounds represents a promising therapeutic strategy, controlling the release of the highly reactive NO remains challenging. Phosphodiesterase 5 (PDE5) inhibitors, like sildenafil, have also been shown to promote wound healing. This study explores hybrid compounds, combining NO-releasing diazeniumdiolates with a sildenafil-derived PDE5 inhibitor. One compound demonstrated a favorable NO-release profile, triggered by an esterase (prodrug), and displayed in vitro nanomolar inhibition potency against PDE5 and thrombin-induced platelet aggregation. Both factors are known to promote blood flow and oxygenation. Thus, our findings unveil promising prospects for effective wound healing treatments.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos Azo / Donantes de Óxido Nítrico / Inhibidores de Fosfodiesterasa 5 Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Alemania
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos Azo / Donantes de Óxido Nítrico / Inhibidores de Fosfodiesterasa 5 Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Alemania