New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CLpro inhibitors

被引：45

作者：

Regnier, Thomas ^{[1
]}

Sarma, Diganta ^{[1
]}

Hidaka, Koushi ^{[1
]}

Bacha, Usman ^{[2
]}

Freire, Ernesto ^{[2
]}

Hayashi, Yoshio ^{[1
,3
]}

Kiso, Yoshiaki ^{[1
]}

机构：

[1] Kyoto Pharmaceut Univ, 21st Century COE Program, Ctr Frontier Res Med Sci, Dept Med Chem, Kyoto 6078412, Japan

[2] Johns Hopkins Univ, Dept Biol, Baltimore, MD 21218 USA

[3] Tokyo Univ Pharm & Life Sci, Sch Pharm, Dept Med Chem, Tokyo 1900392, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 10期

基金：

美国国家卫生研究院; 日本学术振兴会;

关键词：

SARS-CoV; Protease inhibitors; Drug design; Synthesis; 3CL PROTEASE; MAIN PROTEASE; CORONAVIRUS; KETONES; ACID;

D O I：

10.1016/j.bmcl.2009.03.118

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Three candidates had encouraging results for the development of new anti-SARS compounds. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2722 / 2727

页数：6

共 24 条

[1] Coronavirus main proteinase (3CLpro) structure:: Basis for design of anti-SARS drugs [J].

Anand, K ;

Ziebuhr, J ;

Wadhwani, P ;

Mesters, JR ;

Hilgenfeld, R .

SCIENCE, 2003, 300 (5626) :1763-1767

[2] Identification of novel inhibitors of the SARS coronavirus main protease 3CLpro [J].

Bacha, U ;

Barrila, J ;

Velazquez-Campoy, A ;

Leavitt, SA ;

Freire, E .

BIOCHEMISTRY, 2004, 43 (17) :4906-4912

[3] Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors [J].

Chen, LR ;

Wang, YC ;

Lin, YW ;

Chou, SY ;

Chen, SF ;

Liu, LT ;

Wu, YT ;

Chih-Jung, KB ;

Chen, TSS ;

Juang, SH .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (12) :3058-3062

[4]

FROSTEN C, 2003, ENG J MED, V348, P1967

[5] Design and synthesis of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease inhibitors [J].

Ghosh, AK ;

Xi, K ;

Ratia, K ;

Santarsiero, BD ;

Fu, WT ;

Harcourt, BH ;

Rota, PA ;

Baker, SC ;

Johnson, ME ;

Mesecar, AD .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (22) :6767-6771

[6] Structure-based design,synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors [J].

Ghosh, Arun K. ;

Xi, Kai ;

Grum-Tokars, Valerie ;

Xu, Xiaoming ;

Ratia, Kiira ;

Fu, Wentao ;

Houser, Katherine V. ;

Baker, Susan C. ;

Johnson, Michael E. ;

Mesecar, Andrew D. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (21) :5876-5880

[7] Molecular evolution of the SARS coronavirus during the course of the SARS epidemic in China [J].

He, JF ;

Peng, GW ;

Min, J ;

Yu, DW ;

Liang, WJ ;

Zhang, SY ;

Xu, RH ;

Zheng, HY ;

Wu, XW ;

Xu, J ;

Wang, ZH ;

Fang, L ;

Zhang, X ;

Li, H ;

Yan, XG ;

Lu, JH ;

Hu, ZH ;

Huang, JC ;

Wan, ZY ;

Hou, JL ;

Lin, JY ;

Song, HD ;

Wang, SY ;

Zhou, XJ ;

Zhang, GW ;

Gu, BW ;

Zheng, HJ ;

Zhang, XL ;

He, M ;

Zheng, K ;

Wang, BF ;

Fu, G ;

Wang, XN ;

Chen, SJ ;

Chen, Z ;

Hao, P ;

Tang, H ;

Ren, SX ;

Zhong, Y ;

Guo, ZM ;

Liu, Q ;

Miao, YG ;

Kong, XY ;

He, WZ ;

Li, YX ;

Wu, CI ;

Zhao, GP ;

Chiu, RWK ;

Chim, SSC ;

Tong, YK .

SCIENCE, 2004, 303 (5664) :1666-1669

[8] Synthesis and evaluation of keto-glutamine analogues as potent inhibitors of severe acute respiratory syndrome 3CLpro [J].

Jain, RP ;

Pettersson, HI ;

Zhang, JM ;

Aull, KD ;

Fortin, PD ;

Huitema, C ;

Eltis, LD ;

Parrish, JC ;

James, MNG ;

Wishart, DS ;

Vederas, JC .

JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (25) :6113-6116

[9] A novel coronavirus associated with severe acute respiratory syndrome [J].

Ksiazek, TG ;

Erdman, D ;

Goldsmith, CS ;

Zaki, SR ;

Peret, T ;

Emery, S ;

Tong, SX ;

Urbani, C ;

Comer, JA ;

Lim, W ;

Rollin, PE ;

Dowell, SF ;

Ling, AE ;

Humphrey, CD ;

Shieh, WJ ;

Guarner, J ;

Paddock, CD ;

Rota, P ;

Fields, B ;

DeRisi, J ;

Yang, JY ;

Cox, N ;

Hughes, JM ;

LeDuc, JW ;

Bellini, WJ ;

Anderson, LJ .

NEW ENGLAND JOURNAL OF MEDICINE, 2003, 348 (20) :1953-1966

[10] Characterization of SARS main protease and inhibitor assay using a fluorogenic substrate [J].

Kuo, CJ ;

Chi, YH ;

Hsu, JTA ;

Liang, PH .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2004, 318 (04) :862-867

← 1 2 3 →