2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.

Hunt JA; Gonzalez S; Kallashi

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2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.

机译：作为CETP抑制剂的2-芳基苯并恶唑：α-烷氧基酰胺部分的取代和修饰。

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The development of a series of 2-arylbenzoxazole alpha-alkoxyamide and beta-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated alpha-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole beta-alkoxyamine 4 showed a desirable combination of in vitro potency (IC(50)=151 nM) and oral bioavailability in the mouse.

机译：描述了胆固醇酯转移蛋白（CETP）的一系列2-芳基苯并恶唑α-烷氧基酰胺和β-烷氧基胺抑制剂的开发。高度氟化的α-烷氧基酰胺被证明是体外CETP的有效抑制剂，而高度氟化的2-芳基苯并恶唑β-烷氧基胺4在小鼠中显示出体外效价（IC（50）= 151 nM）和口服生物利用度的理想组合。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共4页
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Hunt JA; Gonzalez S; Kallashi;
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1. 2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety. [J] . Hunt JA, Gonzalez S, Kallashi Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：作为CETP抑制剂的2-芳基苯并恶唑：α-烷氧基酰胺部分的取代和修饰。
2. 2-Arylbenzoxazoles as CETP inhibitors: Substitution of the benzoxazole moiety. [J] . Smith CJ, Ali A, Chen Bioorganic and Medicinal Chemistry Letters . 2010,第1期

机译：2-芳基苯并购成为CETP抑制剂：取代苯并恶唑部分。
3. 2-Arylbenzoxazoles as CETP inhibitors: Substitution of the benzoxazole moiety. [J] . Smith CJ, Ali A, Chen Bioorganic and Medicinal Chemistry Letters . 2010,第1期

机译：2-芳基苯并恶唑作为CETP抑制剂：苯并恶唑部分的取代。
4. Discovery of natural products for dual pharmacology CETP inhibitors and niacin receptor agonists [C] . Qiao Lian-sheng, Cai Yi-lian, He Yu-su, International Conference on Systems Biology . 2014

机译：发现具有双重药理学CETP抑制剂和烟酸受体激动剂的天然产物
5. Synthesis of Novel Substituted Acridones as Topoisomerase Inhibitors and Potential Anti-neoplastic Agents [D] . Gurram, Poornima. 2013

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6. Synthesis of and Evaluation of Lipid A Modification by 4-Substituted 4-Deoxy Arabinose Analogs as Potential Inhibitors of Bacterial Polymyxin Resistance [O] . T. Kline, M. S. Trent, C. M. Stead, -1

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7. Synthesis of and evaluation of lipid A modification by 4-substituted 4-deoxy arabinose analogs as potential inhibitors of bacterial polymyxin resistance [O] . T. Kline, M.S. Trent, C.M. Stead, 2008

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8. Nucleophilic Hydroboration of Substituted Styrenes with Lithium Triethylborohydride. A Simple Convenient Procedure for the Markownikoff Hydroboration of Aromatically Conjugated Olefins and the Synthesis of Mixed Organoboranes with the Benzylic (alpha-Arylalkyl) Moiety. [R] . Brown, H. C., Kim, S. C. 1976

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2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.

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