Anti-influenza virus drug design: Sialidase inhibitors

被引:17
作者
Dyason, JC [1 ]
von Itzstein, M [1 ]
机构
[1] Griffith Univ, Ctr Biomol Sci & Drug Discovery, Southport, Qld 9726, Australia
关键词
D O I
10.1071/CH01173
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
This review will give an overview of the design process behind the development of sialidase inhibitors, which can be used as anti-influenza drugs. Two drugs (Relenza(TM) and Tamiflu(TM)) are already available as prescription drugs and a third (BCX-1812) is currently undergoing third-phase clinical trials. Also, the use of molecular-modelling techniques in the understanding of the mechanism and the prediction of inhibition of this enzyme is reviewed.
引用
收藏
页码:663 / 670
页数:8
相关论文
共 57 条
[1]   Synthesis and influenza virus sialidase inhibitory activity of analogues of 4-Guanidino-Neu5Ac2en (Zanamivir) modified in the glycerol side-chain [J].
Andrews, DM ;
Cherry, PC ;
Humber, DC ;
Jones, PS ;
Keeling, SP ;
Martin, PF ;
Shaw, CD ;
Swanson, S .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1999, 34 (7-8) :563-574
[2]   NEW METHOD FOR PREDICTING BINDING-AFFINITY IN COMPUTER-AIDED DRUG DESIGN [J].
AQVIST, J ;
MEDINA, C ;
SAMUELSSON, JE .
PROTEIN ENGINEERING, 1994, 7 (03) :385-391
[3]   Hydrophobic benzoic acids as inhibitors of influenza neuraminidase [J].
Atigadda, VR ;
Brouillette, WJ ;
Duarte, F ;
Babu, YS ;
Bantia, S ;
Chand, P ;
Chu, NM ;
Montgomery, JA ;
Walsh, DA ;
Sudbeck, E ;
Finley, J ;
Air, GM ;
Luo, M ;
Laver, GW .
BIOORGANIC & MEDICINAL CHEMISTRY, 1999, 7 (11) :2487-2497
[4]   Potent inhibition of influenza sialidase by a benzoic acid containing a 2-pyrrolidinone substituent [J].
Atigadda, VR ;
Brouillette, WJ ;
Duarte, F ;
Ali, SM ;
Babu, YS ;
Bantia, S ;
Chand, P ;
Chu, N ;
Montgomery, JA ;
Walsh, DA ;
Sudbeck, EA ;
Finley, J ;
Luo, M ;
Air, GM ;
Laver, GW .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (13) :2332-2343
[5]   BCX-1812 (RWJ-270201): Discovery of a novel, highly potent, orally active, and selective influenza neuraminidase inhibitor through structure-based drug design [J].
Babu, YS ;
Chand, P ;
Bantia, S ;
Kotian, P ;
Dehghani, A ;
El-Kattan, Y ;
Lin, TH ;
Hutchison, TL ;
Elliott, AJ ;
Parker, CD ;
Ananth, SL ;
Horn, LL ;
Laver, GW ;
Montgomery, JA .
JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (19) :3482-3486
[6]   Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir [J].
Bantia, S ;
Parker, CD ;
Ananth, SL ;
Horn, LL ;
Andries, K ;
Chand, P ;
Kotian, PL ;
Dehghani, A ;
El-Kattan, Y ;
Lin, T ;
Hutchison, TL ;
Montgomery, JA ;
Kellog, DL ;
Babu, YS .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2001, 45 (04) :1162-1167
[7]   3-DIMENSIONAL STRUCTURE OF INFLUENZA-A N9 NEURAMINIDASE AND ITS COMPLEX WITH THE INHIBITOR 2-DEOXY 2,3-DEHYDRO-N-ACETYL NEURAMINIC ACID [J].
BOSSARTWHITAKER, P ;
CARSON, M ;
BABU, YS ;
SMITH, CD ;
LAVER, WG ;
AIR, GM .
JOURNAL OF MOLECULAR BIOLOGY, 1993, 232 (04) :1069-1083
[8]   INFLUENZA-B VIRUS NEURAMINIDASE CAN SYNTHESIZE ITS OWN INHIBITOR [J].
BURMEISTER, WP ;
HENRISSAT, B ;
BOSSO, C ;
CUSACK, S ;
RUIGROK, RWH .
STRUCTURE, 1993, 1 (01) :19-26
[9]   THE 2.2-A RESOLUTION CRYSTAL-STRUCTURE OF INFLUENZA-B NEURAMINIDASE AND ITS COMPLEX WITH SIALIC-ACID [J].
BURMEISTER, WP ;
RUIGROK, RWH ;
CUSACK, S .
EMBO JOURNAL, 1992, 11 (01) :49-56
[10]  
CHANDLER M, 1995, J CHEM SOC P1, V9, P1173