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Abstract #70839 Published in IGR 18-2

New furoxan derivatives for the treatment of ocular hypertension

Blangetti M; Rolando B; Chegaev K; Guglielmo S; Lazzarato L; Durante M; Masini E; Almirante N; Bastia E; Impagnatiello F; Fruttero R; Gasco A
Bioorganic and Medicinal Chemistry Letters 2017; 27: 479-483


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 60min 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.

Dipartimento di Scienza e Tecnologia del Farmaco - Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy.

Full article

Classification:

11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
3.8 Pharmacology (Part of: 3 Laboratory methods)



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