Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

Zhang H; Ryono DE; Devasthale P; Wang W; OMalley K; Farrelly D; Gu L; Harrity T; Cap M; Chu C; Locke K; Lippy J; Kunselman L; Morgan N; Flynn N; Moore L; Hosagrahara V; Zhang L; Kadiyala P; Xu C; Doweyko AM; Bell A; Chang C; Muckelbauer J; Zahler R; Hariharan N; Cheng PT

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Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

机译：唑酸作为新型，有效的双PPARα/γ激动剂的设计，合成和结构 - 活性关系。

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The design, synthesis and structure-activity relationships of a novel series of N-phenyl-substituted pyrrole, 1,2-pyrazole and 1,2,3-triazole acid analogs as PPAR ligands are outlined. The triazole acid analogs 3f and 4f were identified as potent dual PPARalpha/gamma agonists both in binding and functional assays in vitro. The 3-oxybenzyl triazole acetic acid analog 3f showed excellent glucose and triglyceride lowering in diabetic db/db mice.

机译：概述了作为PPAR配体作为PPAR配体的新型N-苯基取代的吡咯，1,2-吡唑和1,2,3-三唑酸类似物的设计，合成和结构 - 活性关系。三唑酸类似物3F和4F被鉴定为有效的双抗氨氨氨氨氨氨丙烷/γ激动剂在体外结合和功能性测定。 3-氧苄基三唑乙酸类似物3F在糖尿病DB / DB小鼠中显示出优异的葡萄糖和甘油三酯，降低。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2009年第5期|共6页
作者
Zhang H; Ryono DE; Devasthale P; Wang W; OMalley K; Farrelly D; Gu L; Harrity T; Cap M; Chu C; Locke K; Lippy J; Kunselman L; Morgan N; Flynn N; Moore L; Hosagrahara V; Zhang L; Kadiyala P; Xu C; Doweyko AM; Bell A; Chang C; Muckelbauer J; Zahler R; Hariharan N; Cheng PT;
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Metabolic Diseases Chemistry Bristol-Myers Squibb Research and Development Princeton NJ 08543-5400 USA.;

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1. Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists. [J] . Zhang H, Ryono DE, Devasthale P, Bioorganic and Medicinal Chemistry Letters . 2009,第5期

机译：唑酸作为新型，有效的双PPARα/γ激动剂的设计，合成和结构 - 活性关系。
2. Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists. [J] . Ye XY, Li YX, Farrelly D, Bioorganic and Medicinal Chemistry Letters . 2008,第12期

机译：哌啶和脱氢哌啶羧酸的设计，合成和构效关系是新型有效的双重PPARalpha /γ激动剂。
3. Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists. [J] . Kim NJ, Lee KO, Koo BW, Bioorganic and Medicinal Chemistry Letters . 2007,第13期

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机译：新型谷氨酸受体探针的合成：I. dysiherbaine的全合成，一种有效的谷氨酸受体兴奋性毒素；二。 dysiherbaine类似物的设计和合成；三，取代的苯并噻二叠氮化物的合成及其构效关系及其作为AMPA受体调节剂的作用。
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机译：携带4-噻唑基 - 苯氧基尾部的吲哚乙酸衍生物，一类新的效力PPAR A / G / D锅激动剂：合成，结构 - 活动关系，以及体内疗效

Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

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