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Novel highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulators with pharmacokinetic properties suitable for once-daily oral dosing
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-10-27 , DOI: 10.1016/j.bmcl.2017.10.037 Bharat Lagu , Arthur F. Kluge , Ross A. Fredenburg , Effie Tozzo , Ramesh S. Senaiar , Mahaboobi Jaleel , Sunil K. Panigrahi , Nirbhay K. Tiwari , Narasimha R. Krishnamurthy , Taisuke Takahashi , Michael A. Patane
中文翻译：
具有药代动力学特性的新型高选择性过氧化物酶体增殖物激活受体δ（PPARδ）调节剂，适合于每日一次口服给药
更新日期：2017-10-27
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-10-27 , DOI: 10.1016/j.bmcl.2017.10.037 Bharat Lagu , Arthur F. Kluge , Ross A. Fredenburg , Effie Tozzo , Ramesh S. Senaiar , Mahaboobi Jaleel , Sunil K. Panigrahi , Nirbhay K. Tiwari , Narasimha R. Krishnamurthy , Taisuke Takahashi , Michael A. Patane
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Optimization of benzamide PPARδ modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARδ modulator with significantly improved exposure in multiple species following oral administration.
中文翻译：
具有药代动力学特性的新型高选择性过氧化物酶体增殖物激活受体δ（PPARδ）调节剂，适合于每日一次口服给药
苯甲酰胺PPARδ调节剂1的优化产生了（E）-6-（2-（（（4-（呋喃-2-基）-N-甲基苯甲酰胺基）甲基）苯氧基）-4-甲基己基-4-烯酸（18），一种有效的选择性PPARδ调节剂，在口服后可显着改善多种物质的暴露。
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