Therapeutic uses of prostaglandin F_2¦Á analogues in ocular disease and novel synthetic strategies

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• 作者：Iwona Dams ; Jaromir Wasyluk ; Marek Prost ; Andrzej Kutner
• 关键词：PGF2¦Á analogues ; Side effects ; Glaucoma ; Ocular hypertension ; Prostaglandin synthesis ; Corey lactone
• 刊名：Prostaglandins and Other Lipid Mediators
• 出版年：2013
• 出版时间：July-August, 2013
• 年：2013
• 卷：104-105
• 期：Complete
• 页码：109-121
• 全文大小：980 K

文摘

The pharmacological management of glaucoma and ocular hypertension has significantly changed over the last 18 years with the introduction of PGF_2¦Á analogues, more specifically latanoprost (6), travoprost (8), bimatoprost (10) and tafluprost (12). Prostanoids are currently the first-line medicines among ocular antihypertensive drugs in terms of efficacy, safety, patient compliance and medical economy. Their ability to effectively reduce intraocular pressure with once-per-day dosing, ocular tolerability comparable to timolol and general lack of systemic adverse effects have made them the mainstay of pharmacological therapy for glaucoma and ocular hypertension all over the world. The present review reports a novel, convergent and highly diastereoselective method for the synthesis of PGF_2¦Á analogues from the structurally advanced prostaglandin phenylsulfone (5Z)-(+)-15 and new ¦Ø-chain synthons. The biochemistry, clinical efficacy and side effects of four commercially available PGF_2¦Á analogues, currently used as first-line agents for reducing intraocular pressure in patients with glaucoma or ocular hypertension, are also discussed.