A New Process for the Synthesis of Budesonide 21-Phosphate and Evaluation in a Murine Model of Inflammation
In this study, a new and straightforward process for the preparation of budesonide 21-phosphate (Bud-21P) and its disodium salt (Bud-21P-Na2) is described. The method results in a yield comparable to those obtained by diphosphoryl chloride, but it is more manageable, less expensive, and safer. The new compounds are characterized by better water solubility compared to the parent compound. Moreover, they have been evaluated for their anti-inflammatory activity and the obtained results clearly evidence that Bud-21P and Bud-21P-Na2 retained anti-inflammatory activity like the parent compound budesonide (Bud) in mice with cutaneous induced edema.
Authors
- Vincenzo Santagada (ORCID: https://orcid.org/0000-0001-8377-8990)
- Francesco Petti
- Ferdinando Fiorino (ORCID: https://orcid.org/0000-0001-7357-5751)
- Giuseppe Cirino (ORCID: https://orcid.org/0000-0003-3954-4083)
- Beatrice Ulloa Severino (ORCID: https://orcid.org/0000-0002-3887-8869)
- Francesco Frecentese (ORCID: https://orcid.org/0000-0001-8821-2937)
- Elisa Perissutti (ORCID: https://orcid.org/0000-0002-1754-1191)
- Antonia Scognamiglio (ORCID: https://orcid.org/0000-0002-4282-2788)
- Elisa Magli (ORCID: https://orcid.org/0000-0002-9930-9467)
- Ida Cerqua (ORCID: https://orcid.org/0000-0002-4363-7728)
- Elisabetta Granato (ORCID: https://orcid.org/0000-0002-7207-5832)
- Angela Corvino (ORCID: https://orcid.org/0000-0002-0617-156X)
- Giuseppe Caliendo (ORCID: https://orcid.org/0000-0002-5098-6045)
- Fiorentina Roviezzo (ORCID: https://orcid.org/0000-0003-1582-7396)
- Antonio Petti
- Rocco Pavese
- Francesca Pavese
Institutions
- University of Naples Federico II (IT)
Publication Details
- Journal
- Molecules
- Published
- 2024-09-23
- DOI
- https://doi.org/10.3390/molecules29184514
- Citations
- 1
- Primary Topic
- Natural product bioactivities and synthesis
- Type
- article
- Field-Weighted Citation Impact
- 0.23
Funders
- Ministero della Salute