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gem-Dinitroalkyl Benzenes: A Novel Class of IOP-Lowering Agents for the Treatment of Ocular Hypertension
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-09-15 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00264 Marco Blangetti 1 , Barbara Rolando 1 , Elisabetta Marini 1 , Konstantin Chegaev 1 , Stefano Guglielmo 1 , Loretta Lazzarato 1 , Laura Lucarini 2 , Emanuela Masini 2 , Roberta Fruttero 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-09-15 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00264 Marco Blangetti 1 , Barbara Rolando 1 , Elisabetta Marini 1 , Konstantin Chegaev 1 , Stefano Guglielmo 1 , Loretta Lazzarato 1 , Laura Lucarini 2 , Emanuela Masini 2 , Roberta Fruttero 1
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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.
中文翻译：
宝石-二硝基烷基苯甲酸酯：一类新型的降低眼压的药物，用于治疗眼压过高
原发性开角型青光眼是全世界第二大最常见的失明原因。一氧化氮作为潜在的抗青光眼剂最近受到了特别的关注。在这项工作中，对宝石-二硝基烷基苯作为新型IOP降低剂的能力进行了评估。这些衍生物具有多种NO释放能力，并发现以浓度依赖性方式使收缩的大鼠主动脉条松弛。已经研究了它们在1％剂量的短暂性眼高压兔模型中降低IOP的活性。降低IOP的最有效产品是化合物9 – 11和13，其活性与给药后120分钟的Molsidomine相似。化合物使用卡波姆诱发的青光眼作为IOP的慢性模型，选择9和13进行评估。它们在开始的24小时内导致IOP显着降低，并且其活性维持5天以上，显示出类似Molsidomine的特征。
更新日期：2017-09-15
中文翻译：
宝石-二硝基烷基苯甲酸酯：一类新型的降低眼压的药物，用于治疗眼压过高
原发性开角型青光眼是全世界第二大最常见的失明原因。一氧化氮作为潜在的抗青光眼剂最近受到了特别的关注。在这项工作中，对宝石-二硝基烷基苯作为新型IOP降低剂的能力进行了评估。这些衍生物具有多种NO释放能力，并发现以浓度依赖性方式使收缩的大鼠主动脉条松弛。已经研究了它们在1％剂量的短暂性眼高压兔模型中降低IOP的活性。降低IOP的最有效产品是化合物9 – 11和13，其活性与给药后120分钟的Molsidomine相似。化合物使用卡波姆诱发的青光眼作为IOP的慢性模型，选择9和13进行评估。它们在开始的24小时内导致IOP显着降低，并且其活性维持5天以上，显示出类似Molsidomine的特征。
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