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.

New furoxan derivatives for the treatment of ocular hypertension

BLANGETTI, Marco;ROLANDO, Barbara;CHEGAEV, Konstantin;GUGLIELMO, Stefano;LAZZARATO, Loretta;FRUTTERO, Roberta;GASCO, Alberto
2017

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.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
27
3
479
483
http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistry-letters/
Furoxan; Glaucoma; Nitric oxide; Ocular hypertension; Biochemistry; Molecular Medicine; Molecular Biology; 3003; Drug Discovery3003 Pharmaceutical Science; Clinical Biochemistry; Organic Chemistry
Blangetti, Marco; Rolando, Barbara; Chegaev, Konstantin; Guglielmo, Stefano; Lazzarato, Loretta; Durante, Mariaconcetta; Masini, Emanuela; Almirante, Nicoletta; Bastia, Elena; Impagnatiello, Francesco; Fruttero, Roberta; Gasco, Alberto
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2318/1625289
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