New furoxan derivatives for the treatment of ocular hypertension |
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| Authors: | Marco Blangetti Barbara Rolando Konstantin Chegaev Stefano Guglielmo Loretta Lazzarato Mariaconcetta Durante Emanuela Masini Nicoletta Almirante Elena Bastia Francesco Impagnatiello Roberta Fruttero Alberto Gasco |
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| Affiliation: | 1. Dipartimento di Scienza e Tecnologia del Farmaco – Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy;2. Dipartimento di Neuroscienze, Area del Farmaco e Salute del Bambino (NEUROFARBA) – Università di Firenze, Viale Pieraccini 6, 50139 Firenze (FI), Italy;3. Nicox Research Institute, S.r.l., Via Ludovico Ariosto 21, 20091 Bresso (MI), Italy |
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| Abstract: | 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. |
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| Keywords: | Nitric oxide Furoxan Glaucoma Ocular hypertension |
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