1-(1,3-Benzodioxol-5-ylmethyl)-3-(4-(1H-imidazol-1-yl)phenoxy)-piperidine analogs as potent and selective inhibitors of nitric oxide formation.

Wei RG; Adler M; Davey D; Ho E; Mohan R; Polokoff M; Tseng JL; Whitlow M; Xu W; Yuan S; Phillips G

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >1-(1,3-Benzodioxol-5-ylmethyl)-3-(4-(1H-imidazol-1-yl)phenoxy)-piperidine analogs as potent and selective inhibitors of nitric oxide formation.

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1-(1,3-Benzodioxol-5-ylmethyl)-3-(4-(1H-imidazol-1-yl)phenoxy)-piperidine analogs as potent and selective inhibitors of nitric oxide formation.

机译：1-（1,3-Benzodioxol-5-ylmethyl）-3-（4-（1H-咪唑-1-基）苯氧基）-哌啶类似物是一氧化氮形成的有效和选择性抑制剂。

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A new series of 1-(1,3-benzodioxol-5-ylmethyl)-3-[4-(1H-Imidazol-1-yl)phenoxy]-piperidine analogs were designed and identified as potent and selective inhibitors of NO formation based both on the crystal structure of a murine iNOS Delta114 monomer domain/ inhibitor complex and inhibition of the NO formation in human A172 cell assays. Compound 12S showed high potency and high iNOS selectivity versus nNOS and eNOS.

机译：设计了一系列新的1-（1,3-苯并二恶唑-5-基甲基）-3- [4-（1H-咪唑-1-基）苯氧基]-哌啶类似物，并确定其为有效的和选择性的NO生成抑制剂，基于在鼠iNOS Delta114单体结构域/抑制剂复合物的晶体结构上以及在人类A172细胞分析中抑制NO的形成。与nNOS和eNOS相比，化合物12S显示出高效力和高iNOS选择性。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2007年第9期|共6页
作者
Wei RG; Adler M; Davey D; Ho E; Mohan R; Polokoff M; Tseng JL; Whitlow M; Xu W; Yuan S; Phillips G;
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正文语种 eng
中图分类药学;生物化学;
关键词
inhibitors; analogs; piperidine; Nitric Oxide; structure; 一氧化氮;

机译：抑制剂;类似物;哌啶;一氧化氮;结构;一氧化氮;

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1. 1-(1,3-Benzodioxol-5-ylmethyl)-3-(4-(1H-imidazol-1-yl)phenoxy)-piperidine analogs as potent and selective inhibitors of nitric oxide formation. [J] . Wei RG, Adler M, Davey D, Bioorganic and Medicinal Chemistry Letters . 2007,第9期

机译：1-（1,3-Benzodioxol-5-ylmethyl）-3-（4-（1H-咪唑-1-基）苯氧基）-哌啶类似物是一氧化氮形成的有效和选择性抑制剂。
2. Pharmacological Characterization of SC-57461A (3-[Methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic Acid HCl), a Potent and Selective Inhibitor of Leukotriene A_4 Hydrolase I: In Vitro Studies [J] . Leslie J.Askonas, James F.Kachur, Doreen Villani-Price, The Journal of Pharmacology and Experimental Therapeutics: Official Publication of the American Society for Pharmacology and Experimental Therapeutics . 2002,第2期

机译：白三烯A_4水解酶的强效和选择性抑制剂SC-57461A（3- [甲基[3- [4-（苯基甲基）苯氧基]丙基]氨基]丙酸HCl）的药理特性：体外研究
3. Pharmacological Characterization of SC-57461A (3-[Methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic Acid HCl), a Potent and Selective Inhibitor of Leukotriene A_4 Hydrolase II: In Vivo Studies [J] . James F.Kachur, Leslie J.Askonas, Doreen Villani-Price, The Journal of Pharmacology and Experimental Therapeutics: Official Publication of the American Society for Pharmacology and Experimental Therapeutics . 2002,第2期

机译：白三烯A_4水解酶II的强效和选择性抑制剂SC-57461A（3- [甲基[3- [4-（苯基甲基）苯氧基]丙基]氨基]丙酸HCl）的药理特性：体内研究
4. Synthesis and Characterization of Polyimides from Bis(3-aminophenyl)-4-(1- adamantyl) Phenoxy Phenyl-phosphine Oxide (mDAATPPO) [C] . S. M. Kwak, J. H. Kim, Y. U. Bae PMSE Symposia . 2005

机译：来自双（3-氨基苯基）-4-（1-酰胺基）苯基磷酸氧化膦（MDAATPPO）的聚酰亚胺的合成与表征
5. Hydroxyethylene isosteres as potent and selective inhibitors of neuronal nitric oxide synthase. [D] . Erdal, Erik Paul. 2006

机译：羟乙烯等位基因是神经元一氧化氮合酶的有效和选择性抑制剂。
6. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzoh16naphthyridin-2(1H)-one as a highly potent selective Mammalian Target of Rapamycin (mTOR) inhibitor for the treatment of cancer [O] . Qingsong Liu, Jae Won Chang, Jinhua Wang, -1

机译：1-发现（4-（4- propionylpiperazin -1-基）-3-（三氟甲基）苯基）-9-（喹啉-3-基）苯并h 16萘啶-2（1H） - 一个作为雷帕霉素的高度有效的选择性的哺乳动物靶标（mTOR）抑制剂用于治疗癌症的治疗
7. Discovery of 1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a Highly Potent, Selective Mammalian Target of Rapamycin (mTOR) Inhibitor for the Treatment of Cancer [O] . Liu, Qingsong, Chang, Jae Won, Wang, Jinhua, 2010

机译：发现1-（4-（4-丙酰基哌嗪-1-基）-3-（三氟甲基）苯基）-9-（喹啉-3-基）苯并[h] [1,6]萘啶-2（1H） - 一种作为高效，选择性哺乳动物的雷帕霉素靶蛋白（mTOR）抑制剂治疗癌症

1-(1,3-Benzodioxol-5-ylmethyl)-3-(4-(1H-imidazol-1-yl)phenoxy)-piperidine analogs as potent and selective inhibitors of nitric oxide formation.

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