Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor

被引：8
|
作者：
Webb, TR
Moran, T
Huang, CQ
McCarthy, JR
Grigoriadis, DE
Chen, C
机构：
[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92121 USA
[2] Neurocrine Biosci Inc, Dept Pharmacol, San Diego, CA 92121 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 15期
关键词：
benzoylpyrimidine; CRF; antagonist;
D O I：
10.1016/j.bmcl.2004.05.072
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of benzoylpyrimidines derived from the anilinepyrimidine CRF1 antagonists were synthesized. Several synthetic routes were developed to explore the SAR of this series of compounds. Compounds such as 8d (K-i = 15 nM) exhibited high binding affinities at the human CRF1 receptor. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3869 / 3873
页数：5
相关论文
共 50 条
  • [1] Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists
    Gross, RS
    Guo, ZQ
    Dyck, B
    Coon, T
    Huang, CQ
    Lowe, RF
    Marinkovic, D
    Moorjani, M
    Nelson, J
    Zamani-Kord, S
    Grigoriadis, DE
    Hoare, SRJ
    Crowe, PD
    Bu, JH
    Haddach, M
    McCarthy, J
    Saunders, J
    Sullivan, R
    Chen, TK
    Williams, JP
    JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (18) : 5780 - 5793
  • [2] Corticotropin-releasing factor receptor antagonists
    Gilligan, Paul J.
    EXPERT OPINION ON THERAPEUTIC PATENTS, 2006, 16 (07) : 913 - 924
  • [3] Design and synthesis of tricyclic corticotropin-releasing factor-1 (CRF1) antagonists
    Williams, JP
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 230 : U2511 - U2512
  • [4] Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists
    Mochizuki, Michiyo
    Kori, Masakuni
    Kobayashi, Katsumi
    Yano, Takahiko
    Sako, Yuu
    Tanaka, Maiko
    Kanzaki, Naoyuki
    Gyorkos, Albert C.
    Corrette, Christopher P.
    Cho, Suk Young
    Pratt, Scott A.
    Aso, Kazuyoshi
    JOURNAL OF MEDICINAL CHEMISTRY, 2016, 59 (06) : 2551 - 2566
  • [5] Corticotropin-releasing factor 1 receptor antagonists: a patent review
    Williams, John P.
    EXPERT OPINION ON THERAPEUTIC PATENTS, 2013, 23 (08) : 1057 - 1068
  • [6] Chiral separation of potent corticotropin-releasing factor-1 receptor antagonists by supercritical fluid chromatography
    Qian-Cutrone, Jingfang
    Hartz, Richard
    Ahuja, Vijay T.
    Vrudhula, Vivekananda M.
    Wu, Dauh-Rurng
    Dalterio, Richard A.
    Wang-Iverson, David
    Bronson, Joanne J.
    JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2011, 54 (03) : 602 - 606
  • [7] Neuroprotective effects of corticotropin-releasing factor receptor antagonists
    Loddick, SA
    Chalmers, DT
    Yatsushiro, K
    McCulloch, J
    Foster, AC
    Rothwell, NJ
    De Souza, EB
    PHARMACOLOGY OF CEREBRAL ISCHEMIA 1998, 1999, : 371 - 378
  • [8] Recent Advances in Corticotropin-Releasing Factor Receptor Antagonists
    Dzierba, Carolyn D.
    Hartz, Richard A.
    Bronson, Joanne J.
    ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 43, 2008, 43 : 3 - 23
  • [9] Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists
    Lowe, RF
    Nelson, J
    Dang, TN
    Crowe, PD
    Pahuja, A
    McCarthy, JR
    Grigoriadis, DE
    Conlon, P
    Saunders, J
    Chen, C
    Szabo, T
    Chen, TK
    Bozigian, H
    JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (05) : 1540 - 1549
  • [10] Synthesis and SAR of 8-aza-quinoxalin-2(1H)-one as corticotropin-releasing factor-1 receptor antagonists
    Dasgupta, Bireshwar
    Dzierba, Carolyn D.
    Sielecki, Thais M.
    Galka, Amy
    Johnson, Tricia L.
    Takvorian, Amy G.
    Rafalski, Maria
    Kasireddy-Polam, Padmaja
    Vig, Shikha
    Arvanitis, Argyrios G.
    Zhang, Ge
    Molski, Thaddeus F.
    Zaczek, Robert C.
    Combs, Andrew P.
    Gilligan, Paul J.
    Trainor, George
    Bronson, Joanne J.
    Macor, John E.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2009, 238
12345