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ACS Med Chem Lett. 2017 Sep 13;8(10):1054-1059. doi: 10.1021/acsmedchemlett.7b00264. eCollection 2017.

gem-Dinitroalkyl Benzenes: A Novel Class of IOP-Lowering Agents for the Treatment of Ocular Hypertension.

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  • 1Dipartimento di Scienza e Tecnologia del Farmaco, Universit√† degli Studi di Torino, Via P. Giuria 9, 10125 Turin, Italy.
  • 2Dipartimento di Neuroscienze, Area del Farmaco e Salute del Bambino (NEUROFARBA), Universit√† di Firenze, Viale Pieraccini 6, 50139 Florence (FI), Italy.


Primary open angle glaucoma is the second most common cause of blindness worldwide. Nitric oxide has recently received particular attention as a potential antiglaucoma agent. In this work, gem-dinitroalkyl benzenes are evaluated for their capability to act as a new class of IOP lowering agents. These derivatives have been endowed with a variety of NO-release capacities and found to relax contracted rat aorta strips in a concentration-dependent manner. They have been studied for their IOP-lowering activity in a transient ocular hypertensive rabbit model at 1% dose. The most effective IOP-lowering products were compounds 9-11 and 13, whose activity was similar to that of Molsidomine 120 min after administration. Compounds 9 and 13 were selected for evaluation using carbomer-induced glaucoma as the chronic model of IOP. They cause a significant reduction in IOP in the first 24 h, and their activity is maintained over 5 days, displaying a Molsidomine-like profile.


gem-Dinitroalkyl benzenes; glaucoma; nitric oxide; ocular hypertension

[Available on 2018-10-12]
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