Synthesis, docking studies, and evaluation of pyrimidines as inhibitors of SARS-CoV 3CL protease

被引:52
|
作者
Ramajayam, R. [1 ]
Tan, Kian-Pin [2 ]
Liu, Hun-Ge [2 ]
Liang, Po-Huang [1 ,2 ]
机构
[1] Acad Sinica, Inst Biol Chem, Taipei 11529, Taiwan
[2] Natl Taiwan Univ, Inst Biochem Sci, Taipei 106, Taiwan
关键词
SARS-CoV; Pyrimidines; RESPIRATORY SYNDROME CORONAVIRUS; MAIN PROTEASE; IDENTIFICATION; DESIGN; DERIVATIVES; CINANSERIN; ANALOGS;
D O I
10.1016/j.bmcl.2010.04.118
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 2-(benzylthio)-6-oxo-4-phenyl-1,6-dihydropyrimidine as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Two candidates had encouraging results for the development of new anti-SARS compounds. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3569 / 3572
页数:4
相关论文
共 50 条
  • [1] Synthesis and Evaluation of Benzoquinolinone Derivatives as SARS-CoV 3CL Protease Inhibitors
    Ahn, Tae-Young
    Kuo, Chih-Jung
    Liu, Hun-Ge
    Ha, Deok-Chan
    Liang, Po-Huang
    Jung, Young-Sik
    [J]. BULLETIN OF THE KOREAN CHEMICAL SOCIETY, 2010, 31 (01): : 87 - 91
  • [2] Preparation of SARS-CoV 3CL Protease and Synthesis of its Inhibitors
    Konno, Hiroyuki
    Akaji, Kenichi
    [J]. JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY JAPAN, 2021, 79 (01) : 2 - 10
  • [3] Design, synthesis, and evaluation of trifluoromethyl ketones as inhibitors of SARS-CoV 3CL protease
    Shao, Yi-Ming
    Yang, Wen-Bin
    Kuo, Tun-Hsun
    Tsai, Keng-Chang
    Lin, Chun-Hung
    Yang, An-Suei
    Liang, Po-Huang
    Wong, Chi-Huey
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (08) : 4652 - 4660
  • [4] Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor
    Konno, Hiroyuki
    Onuma, Takumi
    Nitanai, Ikumi
    Wakabayashi, Masaki
    Yano, Shigekazu
    Teruya, Kenta
    Akaji, Kenichi
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (12) : 2746 - 2751
  • [5] Evaluation of metal-conjugated compounds as inhibitors of 3CL protease of SARS-CoV
    Hsu, JTA
    Kuo, CJ
    Hsieh, HP
    Wang, YC
    Huang, KK
    Lin, CPC
    Huang, PF
    Chen, X
    Liang, PH
    [J]. FEBS LETTERS, 2004, 574 (1-3): : 116 - 120
  • [6] Inhibition of SARS-CoV 3CL protease by flavonoids
    Jo, Seri
    Kim, Suwon
    Shin, Dong Hae
    Kim, Mi-Sun
    [J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2020, 35 (01) : 145 - 151
  • [7] Structure-based design and synthesis of highly potent SARS-CoV 3CL protease inhibitors
    Shao, Yi-Ming
    Yang, Wen-Bin
    Peng, Hung-Pin
    Hsu, Min-Feng
    Tsa, Keng-Chang
    Kuo, Tun-Hsun
    Wang, Andrew H. -J.
    Liang, Po-Huang
    Lin, Chun-Hung
    Yang, An-Suei
    Wong, Chi-Huey
    [J]. CHEMBIOCHEM, 2007, 8 (14) : 1654 - 1657
  • [8] Development of potent dipeptide-type SARS-CoV 3CL protease inhibitors with novel P3 scaffolds: Design, synthesis, biological evaluation, and docking studies
    Thanigaimalai, Pillaiyar
    Konno, Sho
    Yamamoto, Takehito
    Koiwai, Yuji
    Taguchi, Akihiro
    Takayama, Kentaro
    Yakushiji, Fumika
    Akaji, Kenichi
    Chen, Shen-En
    Naser-Tavakolian, Aurash
    Schoen, Arne
    Freire, Ernesto
    Hayashi, Yoshio
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 68 : 372 - 384
  • [9] Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease
    Liu, YC
    Huang, V
    Chao, TC
    Hsiao, CD
    Lin, A
    Chang, MF
    Chow, LP
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2005, 333 (01) : 194 - 199
  • [10] Mechanism of the maturation process of SARS-CoV 3CL protease
    Hsu, MF
    Kuo, CJ
    Chang, KT
    Chang, HC
    Chou, CC
    Ko, TP
    Shr, HL
    Chang, GG
    Wang, AHJ
    Liang, PH
    [J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 2005, 280 (35) : 31257 - 31266