Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1

被引：30

作者：

Wu, Tom Y. H. ^{[1
]}

Juteau, Helene ^{[1
]}

Ducharme, Yves ^{[1
]}

Friesen, Richard W. ^{[1
]}

Guiral, Sebastien ^{[1
]}

Dufresne, Lynn ^{[1
]}

Poirier, Hugo ^{[1
]}

Salem, Myriam ^{[1
]}

Riendeau, Denis ^{[1
]}

Mancini, Joseph ^{[1
]}

Brideau, Christine ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Kirkland, PQ H9H 3L1, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 23期

关键词：

mPGES-1; Inhibitor; Biarylimidazole; PGE2; Inflammation; CYCLOOXYGENASE-2; MPGES-1; AGENTS; ASSAY;

D O I：

10.1016/j.bmcl.2010.09.129

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：6978 / 6982

页数：5

共 50 条

[41] Microsomal prostaglandin E synthase-1 in rheumatic diseases
Korotkova, Marina
Jakobsson, Per-Johan
[J]. FRONTIERS IN PHARMACOLOGY, 2011, 1
[42] Cardiovascular Biology of Microsomal Prostaglandin E Synthase-1
Wang, Miao
FitzGerald, Garret A.
[J]. TRENDS IN CARDIOVASCULAR MEDICINE, 2010, 20 (06) : 189 - 195
[43] Microsomal prostaglandin E synthase-1 contributes to ischaemic excitotoxicity through prostaglandin E2 EP3 receptors
Ikeda-Matsuo, Y.
Tanji, H.
Ota, A.
Hirayama, Y.
Uematsu, S.
Akira, S.
Sasaki, Y.
[J]. BRITISH JOURNAL OF PHARMACOLOGY, 2010, 160 (04) : 847 - 859
[44] Discovery of N-amido-phenylsulfonamide derivatives as novel microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors
Kim, Misong
Kim, Geuntae
Kang, Minji
Ko, Dohyeong
Nam, Yunchan
Moon, Chang Sang
Kang, Heung Mo
Shin, Ji-Sun
Werz, Oliver
Lee, Kyung-Tae
Lee, Jae Yeol
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021, 41
[45] Identification of novel microsomal prostaglandin E2 synthase-1 (mPGES-1) lead inhibitors from Fragment Virtual Screening
Lauro, Gianluigi
Manfra, Michele
Pedatella, Silvana
Fischer, Katrin
Cantone, Vincenza
Terracciano, Stefania
Bertamino, Alessia
Ostacolo, Carmine
Gomez-Monterrey, Isabel
De Nisco, Mauro
Riccio, Raffaele
Novellino, Ettore
Werz, Oliver
Campiglia, Pietro
Bifulco, Giuseppe
[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2017, 125 : 278 - 287
[46] Exogenous Prostaglandin E2 And E-Prostanoid-2 Receptor Agonist Stimulate Microsomal Prostaglandin E Synthase-1 In Lung Fibroblasts
Gunji, Y.
Sato, T.
Ikari, J.
Iwasawa, S.
Kanaji, N.
Nelson, A.
Togo, S.
Park, J.
Farid, M.
Michalski, J.
Wang, X.
Basma, H.
Liu, X.
Feghali-Bostwick, C.
Rennard, S. I.
[J]. AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, 2013, 187
[47] Glucosamine Sulphate Reduces the Prostaglandin E2 Production In Osteoarthritic Cartilage Through the Inhibition of Microsomal Prostaglandin E Synthase-1
Kapoor, Mohit
Mineau, Francois
Fahmi, Hassan
Pelletier, Jean Pierre
Martel-Pelletier, Johanne
[J]. ARTHRITIS AND RHEUMATISM, 2011, 63 (10): : S23 - S24
[48] Discovery of Depsides and Depsidones from Lichen as Potent Inhibitors of Microsomal Prostaglandin E2 Synthase-1 Using Pharmacophore Models
Bauer, Julia
Waltenberger, Birgit
Noha, Stefan M.
Schuster, Daniela
Rollinger, Judith M.
Boustie, Joel
Chollet, Marylene
Stuppner, Hermann
Werz, Oliver
[J]. CHEMMEDCHEM, 2012, 7 (12) : 2077 - 2081
[49] Perspective of microsomal prostaglandin E2 synthase-1 as drug target in inflammation-related disorders
Koeberle, Andreas
Werz, Oliver
[J]. BIOCHEMICAL PHARMACOLOGY, 2015, 98 (01) : 1 - 15
[50] Microsomal Prostaglandin E2 Synthase-1 as a New Macromolecular Drug Target in the Prevention of Inflammation and Cancer
Bulbul, Bahadir
Kucukguzel, Ilkay
[J]. ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2019, 19 (10) : 1205 - 1222

← 1 2 3 4 5 →