New furoxan derivatives for the treatment of ocular hypertension
| Autor: | Francesco Impagnatiello, Loretta Lazzarato, Elena Bastia, Nicoletta Almirante, Alberto Gasco, Barbara Rolando, Marco Blangetti, Emanuela Masini, Stefano Guglielmo, Roberta Fruttero, Konstantin Chegaev, Mariaconcetta Durante |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
genetic structures Clinical Biochemistry Pharmaceutical Science Timolol Ocular hypertension Pharmacology Clinical biochemistry Biochemistry Nitric oxide 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Furoxan Glaucoma Molecular Medicine Molecular Biology 3003 Drug Discovery3003 Pharmaceutical Science Organic Chemistry Drug Discovery medicine Animals Antihypertensive Agents Intraocular Pressure Oxadiazoles medicine.disease eye diseases Disease Models Animal 030104 developmental biology Solubility chemistry 030221 ophthalmology & optometry Rabbit model Rabbits High intraocular pressure medicine.drug |
| Popis: | A small series of water-soluble NO-donor furoxans bearing a basic center at the 4-position, having a wide lipophilic-hydrophilic balance range, and endowed with different NO-release capacities, were synthesized and characterized. Selected members were studied for their IOP-lowering activity in the transient ocular hypertensive rabbit model at 1% dose. The most effective IOP-lowering products were compounds 3 and 7, whose activity 60 min after administration was similar to that of Timolol. Notably, 7 was characterized by a long-lasting action. The IOP-lowering activity in this series of products appeared to be modulated by the lipophilic-hydrophilic balance rather than by the NO-donor capacity. |
| Databáze: | OpenAIRE |
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