title: New furoxan derivatives for the treatment of ocular hypertension.
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 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.
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco - Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy.
authors.forename: Marco
authors.initials: M
authors.lastname: Blangetti
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco - Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy.
authors.forename: Barbara
authors.initials: B
authors.lastname: Rolando
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco - Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy.
authors.forename: Konstantin
authors.initials: K
authors.lastname: Chegaev
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco - Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Guglielmo
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco - Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy. Electronic address: loretta.lazzarato@unito.it.
authors.forename: Loretta
authors.initials: L
authors.lastname: Lazzarato
authors.affiliation: Dipartimento di Neuroscienze, Area del Farmaco e Salute del Bambino (NEUROFARBA) - Università di Firenze, Viale Pieraccini 6, 50139 Firenze (FI), Italy.
authors.forename: Mariaconcetta
authors.initials: M
authors.lastname: Durante
authors.affiliation: Dipartimento di Neuroscienze, Area del Farmaco e Salute del Bambino (NEUROFARBA) - Università di Firenze, Viale Pieraccini 6, 50139 Firenze (FI), Italy.
authors.forename: Emanuela
authors.initials: E
authors.lastname: Masini
authors.affiliation: Nicox Research Institute, S.r.l., Via Ludovico Ariosto 21, 20091 Bresso (MI), Italy.
authors.forename: Nicoletta
authors.initials: N
authors.lastname: Almirante
authors.affiliation: Nicox Research Institute, S.r.l., Via Ludovico Ariosto 21, 20091 Bresso (MI), Italy.
authors.forename: Elena
authors.initials: E
authors.lastname: Bastia
authors.affiliation: Nicox Research Institute, S.r.l., Via Ludovico Ariosto 21, 20091 Bresso (MI), Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Impagnatiello
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco - Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy.
authors.forename: Roberta
authors.initials: R
authors.lastname: Fruttero
authors.affiliation: Dipartimento di Scienza e Tecnologia del Farmaco - Università degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy.
authors.forename: Alberto
authors.initials: A
authors.lastname: Gasco
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D004195:Disease Models, Animal; D005901:Glaucoma / Q000188:drug therapy; D007429:Intraocular Pressure / Q000187:drug effects; D009569:Nitric Oxide / Q000378:metabolism; D009798:Ocular Hypertension / Q000188:drug therapy / Q000473:pathology; D010069:Oxadiazoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D011817:Rabbits; D012995:Solubility; D013999:Timolol / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000959:Antihypertensive Agents; D010069:Oxadiazoles; C010166:furoxans; D009569:Nitric Oxide; D013999:Timolol
keywords: Furoxan; Glaucoma; Nitric oxide; Ocular hypertension