Sar in the alkoxy lactone series:: The discovery of DFP, a potent and orally active COX-2 inhibitor

被引：49
|
作者：
Leblanc, Y
Roy, P
Boyce, S
Brideau, C
Chan, CC
Charleson, S
Gordon, R
Grimm, E
Guay, J
Léger, S
Li, CS
Riendeau, D
Visco, D
Wang, Z
Webb, J
Xu, LJ
Prasit, P
机构：
[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada
[2] Merck Res Labs, Harlow, Essex, England
[3] Merck Res Labs, Rahway, NJ USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 15期
关键词：
D O I：
10.1016/S0960-894X(99)00365-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2-(5H)-furanone), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2207 / 2212
页数：6
相关论文
共 50 条
  • [31] Discovery and characterization of a novel potent, selective and orally active inhibitor for mammalian ELOVL6
    Shimamura, Ken
    Nagumo, Akira
    Miyamoto, Yasuhisa
    Kitazawa, Hidefumi
    Kanesaka, Maki
    Yoshimoto, Ryo
    Aragane, Katsumi
    Morita, Naomi
    Ohe, Tomoyuki
    Takahashi, Toshiyuki
    Nagase, Tsuyoshi
    Sato, Nagaaki
    Tokita, Shigeru
    EUROPEAN JOURNAL OF PHARMACOLOGY, 2010, 630 (1-3) : 34 - 41
  • [32] Novel 1,2-diarylcyclobutenes: Selective and orally active COX-2 inhibitors
    Friesen, RW
    Dube, D
    Fortin, R
    Frenette, R
    Prescott, S
    Cromlish, W
    Greig, GM
    Kargman, S
    Wong, E
    Chan, CC
    Gordon, R
    Xu, LJ
    Riendeau, D
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (22) : 2677 - 2682
  • [33] Synthesis and SAR of 2-aryloxy-4-alkoxy-pyridines as potent orally active corticotropin-releasing factor 1 receptor antagonists
    Chen, Yuhpyng L.
    Braselton, John
    Forman, James
    Gallaschun, Randall J.
    Mansbach, Robert
    Schmidt, Anne W.
    Seeger, Thomas F.
    Sprouse, Jeff S.
    Tingley, F. David, III
    Winston, Elizabeth
    Schulz, David W.
    JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (05) : 1377 - 1384
  • [34] Discovery of a novel, potent and orally active series of γ-lactams as selective NK1 antagonists
    Paliwal, Sunil
    Reichard, Gregory A.
    Shah, Sapna
    Wrobleski, Michelle Laci
    Wang, Cheng
    Stengone, Carmine
    Tsui, Hon-Chung
    Xiao, Dong
    Duffy, Ruth A.
    Lachowicz, Jean E.
    Nomeir, Amin A.
    Varty, Geoffrey B.
    Shih, Neng-Yang
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (14) : 4168 - 4171
  • [35] Discovery of UR-8880:: A new COX-2 selective inhibitor.
    Almansa, C
    Alfon, J
    Cavalcanti, FL
    Escamilla, I
    Gómez, L
    Miralles, A
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 222 : U686 - U686
  • [36] In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor
    Li, J
    Lynch, MP
    DeMello, KL
    Sakya, SM
    Cheng, HM
    Rafka, RJ
    Bronk, BS
    Jaynes, BH
    Kilroy, C
    Mann, DW
    Haven, ML
    Kolosko, NL
    Petras, C
    Seibel, SB
    Lund, LA
    BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (05) : 1805 - 1809
  • [37] Ex vivo assays demonstrate potency and selectivity of the COX-2 inhibitor DFP after single dose administration
    A. Dallob
    I. De Lepeleire
    A. Van Hecken
    A. Porras
    M. Depré
    S. Mukhopadhyay
    M. Flynn
    L. Wildonger
    K. Gottesdiener
    W. Tanaka
    P. De Schepper
    Inflammation Research, 1999, 48 (Suppl 2) : 130 - 131
  • [38] Ex vivo assays demonstrate potency and selectivity of the COX-2 inhibitor DFP after single dose administration
    Dallob, A
    De Lepeleire, I
    Van Hecken, A
    Porras, A
    Depré, M
    Mukhopadhyay, S
    Flynn, M
    Wildonger, L
    Gottesdiener, K
    Tanaka, W
    De Schepper, P
    INFLAMMATION RESEARCH, 1999, 48 : S130 - S131
  • [39] An efficient asymmetric synthesis of a potent COX-2 inhibitor L-784,512
    Tan, LS
    Chen, CY
    Larsen, RD
    Verhoeven, TR
    Reider, PJ
    TETRAHEDRON LETTERS, 1998, 39 (23) : 3961 - 3964
  • [40] A potent dual inhibitor targeting COX-2 and HDAC of acute myeloid leukemia cells
    Qin, Xiang
    Wang, Xueting
    Yang, Chunmei
    Wang, Fan
    Fang, Tingting
    Gu, Didi
    Guo, Qulian
    Meng, Qiuyu
    Liu, Wenjun
    Yang, Lu
    MOLECULAR DIVERSITY, 2024,
12345