Synthesis of 5,6-dihydro-4-hydroxy-2-pyrones as HIV-1 protease inhibitors: The profound effect of polarity on antiviral activity

被引:60
作者
Hagen, SE
Prasad, JVNV
Boyer, FE
Domagala, JM
Ellsworth, EL
Gajda, C
Hamilton, HW
Markoski, LJ
Steinbaugh, BA
Tait, BD
Lunney, EA
Tummino, PJ
Ferguson, D
Hupe, D
Nouhan, C
Gracheck, SJ
Saunders, JM
VanderRoest, S
机构
[1] PARKE DAVIS PHARMACEUT RES,DEPT BIOMOL STRUCT & DRUG DESIGN,ANN ARBOR,MI 48105
[2] PARKE DAVIS PHARMACEUT RES,DEPT BIOCHEM,ANN ARBOR,MI 48105
[3] PARKE DAVIS PHARMACEUT RES,DEPT INFECT DIS,ANN ARBOR,MI 48105
关键词
D O I
10.1021/jm970522y
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
[No abstract available]
引用
收藏
页码:3707 / 3711
页数:5
相关论文
共 21 条
[1]   Protease inhibitors in patients with HIV disease - Clinically important pharmacokinetic considerations [J].
Barry, M ;
Gibbons, S ;
Back, D ;
Mulcahy, F .
CLINICAL PHARMACOKINETICS, 1997, 32 (03) :194-209
[2]   THIAZOLOBENZIMIDAZOLE - BIOLOGICAL AND BIOCHEMICAL ANTIRETROVIRAL ACTIVITY OF A NEW NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITOR [J].
BUCKHEIT, RW ;
HOLLINGSHEAD, MG ;
GERMANYDECKER, J ;
WHITE, EL ;
MCMAHON, JB ;
ALLEN, LB ;
ROSS, LJ ;
DECKER, WD ;
WESTBROOK, L ;
SHANNON, WM ;
WEISLOW, O ;
BADER, JP ;
BOYD, MR .
ANTIVIRAL RESEARCH, 1993, 21 (03) :247-265
[3]   Recent developments in HIV protease inhibitor research [J].
Chrusciel, RA ;
Romines, KR .
EXPERT OPINION ON THERAPEUTIC PATENTS, 1997, 7 (02) :111-121
[4]   HIV-1 protease inhibitors - A review for clinicians [J].
Deeks, SG ;
Smith, M ;
Holodniy, M ;
Kahn, JO .
JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION, 1997, 277 (02) :145-153
[5]   THE NOT-SO-GREAT ESCAPE [J].
ERICKSON, JW .
NATURE STRUCTURAL BIOLOGY, 1995, 2 (07) :523-529
[6]   Viral dynamics of HIV: Implications for drug development and therapeutic strategies [J].
Havlir, DV ;
Richman, DD .
ANNALS OF INTERNAL MEDICINE, 1996, 124 (11) :984-994
[7]  
LELAND J, 1996, NEWSWEEK 1202, P65
[8]  
MASCOLINI M, 1996, J INT ASS PHYSICIANS, V4, P23
[9]   Current knowledge and future prospects for the use of HIV protease inhibitors [J].
Moyle, G ;
Gazzard, B .
DRUGS, 1996, 51 (05) :701-712
[10]   CONVERSION OF PHENOLS TO THIOPHENOLS VIA DIALKYLTHIOCARBAMATES [J].
NEWMAN, MS ;
KARNES, HA .
JOURNAL OF ORGANIC CHEMISTRY, 1966, 31 (12) :3980-&