New furoxan derivatives for the treatment of ocular hypertension. Issue 3 (1st February 2017)

• Record Type: Journal Article
• Authors: Blangetti, Marco; Rolando, Barbara; Chegaev, Konstantin; Guglielmo, Stefano; Lazzarato, Loretta; Durante, Mariaconcetta; Masini, Emanuela; Almirante, Nicoletta; Bastia, Elena; Impagnatiello, Francesco; Fruttero, Roberta; Gasco, Alberto
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 3(2017)
• Page Start: 479
• Page End: 483
• Publication Date: 2017-02-01
• Subjects: Nitric oxide -- Furoxan -- Glaucoma -- Ocular hypertension; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.12.041
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 compounds3 and7, 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.