Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1.

Wu TY; Juteau H; Ducharme Y; Friesen RW; Guiral S; Dufresne L; Poirier H; Salem M; Riendeau D; Mancini J; Brideau C

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Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1.

机译：Biarylimidazoles作为微粒体前列腺素E2合酶1的抑制剂。

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Microsomal prostaglandin E(2) synthase (mPGES-1) represents a potential target for novel analgesic and anti-inflammatory agents. High-throughput screening identified several leads of mPGES-1 inhibitors which were further optimized for potency and selectivity. A series of inhibitors bearing a biaryl imidazole scaffold exhibits excellent inhibition of PGE(2) production in enzymatic and cell-based assays. The synthesis of these molecules and their activities will be discussed.

机译：微粒体前列腺素E（2）合酶（mPGES-1）代表新型镇痛药和抗炎药的潜在目标。高通量筛选确定了mPGES-1抑制剂的几条线索，并对其效力和选择性进行了进一步优化。一系列带有联芳基咪唑支架的抑制剂在酶法和基于细胞的测定法中表现出对PGE（2）产生的优异抑制作用。将讨论这些分子的合成及其活性。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第23期|共5页
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Wu TY; Juteau H; Ducharme Y; Friesen RW; Guiral S; Dufresne L; Poirier H; Salem M; Riendeau D; Mancini J; Brideau C;
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1. Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1. [J] . Wu TY, Juteau H, Ducharme Y, Bioorganic and Medicinal Chemistry Letters . 2010,第23期

机译：Biarylimidazoles作为微粒体前列腺素E2合酶1的抑制剂。
2. Pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1. [J] . Andrea Wiegard, Walburga Hanekamp, Klaus Griessbach, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2012,第2期

机译：吡咯烷酸衍生物作为微粒体前列腺素E2合酶1的有害抑制剂。
3. Pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1. [J] . Andrea Wiegard, Walburga Hanekamp, Klaus Griessbach, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2012,第1期

机译：吡咯烷酸衍生物作为微粒体前列腺素E2合酶1的有害抑制剂。
4. Synthesis, In Silico Molecular Docking Modeling and Pharmacophore Mapping of (E)-3-(4-Hydroxy-2,6-Dimethoxyphenyl)-1 -Phenylprop-2-en-1 - One as Potential New Inhibitor of Microsomal Prostaglandin E2 Synthase-1 [C] . Pitipat Sanphetchaloemchok, Mohd Fadhlizil Fasihi Mohd Aluwi, Kamal Rullah, Postgraduate Symposium on Industrial Science and Technology . 2020

机译：（E）-3-（4-羟基-2,6-二甲氧基苯基）-1-phenylprop-2-en-1的硅分子对接建模和药效线映射，作为微粒体前列腺素E2合酶的潜在新抑制剂 - 1
5. Discovery and characterization of novel inhibitors of the prostaglandin E2 pathway. [D] . Chang, Hui-Hua. 2013

机译：发现和表征前列腺素E2途径的新型抑制剂。
6. Hyperforin an Anti-Inflammatory Constituent from St. Johns Wort Inhibits Microsomal Prostaglandin E2 Synthase-1 and Suppresses Prostaglandin E2 Formation in vivo [O] . Andreas Koeberle, Antonietta Rossi, Julia Bauer, 2011

机译：Hyperforin是一种来自圣约翰草的抗炎成分抑制微粒体前列腺素E2合酶1并抑制体内前列腺素E2的形成。
7. Hyperforin, an Anti-Inflammatory Constituent from St. John's Wort, Inhibits Microsomal Prostaglandin E2 Synthase-1 and Suppresses Prostaglandin E2 Formation in vivo [O] . Koeberle, Andreas, Rossi, Antonietta, Bauer, Julia, 2011

机译：Hyperforin是一种来自圣约翰草的抗炎成分，抑制微粒体前列腺素E2合酶1并抑制体内前列腺素E2的形成。

Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1.

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