POTENT HIV-1 PROTEASE INHIBITORS WITH ANTIVIRAL ACTIVITIES INVITRO

被引：22

作者：

SHAM, HL

BETEBENNER, DA

WIDEBURG, NE

SALDIVAR, AC

KOHLBRENNER, WE

VASAVANONDA, S

KEMPF, DJ

NORBECK, DW

ZHAO, C

CLEMENT, JJ

ERICKSON, JE

PLATTNER, JJ

机构：

[1] Abbott Laboratories, Pharmaceutical Discovery Division, Abbott Park

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1991年 / 175卷 / 03期

关键词：

D O I：

10.1016/0006-291X(91)91652-S

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel difluoroketones with low molecular weight (<600 m.u.) and which are potent inhibitors of the HIV-1 protease (IC50=1.0 to 21 nM) were synthesized. These compounds also exhibited antiviral activity by inhibition of the cytopathic effect of HIV-13B in MT-4 cells in vitro. © 1991.

引用

页码：914 / 919

页数：6

共 20 条

[1] INHIBITION OF HUMAN IMMUNODEFICIENCY VIRUS-1 PROTEASE INVITRO - RATIONAL DESIGN OF SUBSTRATE-ANALOG INHIBITORS [J].

DREYER, GB ;

METCALF, BW ;

TOMASZEK, TA ;

CARR, TJ ;

CHANDLER, AC ;

HYLAND, L ;

FAKHOURY, SA ;

MAGAARD, VW ;

MOORE, ML ;

STRICKLER, JE ;

DEBOUCK, C ;

MEEK, TD .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1989, 86 (24) :9752-9756

[2]

GALLINA C, 1989, SYNTHESIS-STUTTGART, P466

[3] FLUORO KETONE INHIBITORS OF HYDROLYTIC ENZYMES [J].

GELB, MH ;

SVAREN, JP ;

ABELES, RH .

BIOCHEMISTRY, 1985, 24 (08) :1813-1817

[4] STRUCTURE-BASED, C2 SYMMETRICAL INHIBITORS OF HIV PROTEASE [J].

KEMPF, DJ ;

NORBECK, DW ;

CODACOVI, LM ;

WANG, XC ;

KOHLBRENNER, WE ;

WIDEBURG, NE ;

PAUL, DA ;

KNIGGE, MF ;

VASAVANONDA, S ;

CRAIGKENNARD, A ;

SALDIVAR, A ;

ROSENBROOK, W ;

CLEMENT, JJ ;

PLATTNER, JJ ;

ERICKSON, J .

JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (10) :2687-2689

[5]

KEMPF DJ, 1990, Patent No. 402646

[6] ACTIVE HUMAN IMMUNODEFICIENCY VIRUS PROTEASE IS REQUIRED FOR VIRAL INFECTIVITY [J].

KOHL, NE ;

EMINI, EA ;

SCHLEIF, WA ;

DAVIS, LJ ;

HEIMBACH, JC ;

DIXON, RAF ;

SCOLNICK, EM ;

SIGAL, IS .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1988, 85 (13) :4686-4690

[7] HTLV-III GAG PROTEIN IS PROCESSED IN YEAST-CELLS BY THE VIRUS POL-PROTEASE [J].

KRAMER, RA ;

SCHABER, MD ;

SKALKA, AM ;

GANGULY, K ;

WONGSTAAL, F ;

REDDY, EP .

SCIENCE, 1986, 231 (4745) :1580-1584

[8] NOVEL FLUOROGENIC SUBSTRATES FOR ASSAYING RETROVIRAL PROTEASES BY RESONANCE ENERGY-TRANSFER [J].

MATAYOSHI, ED ;

WANG, GT ;

KRAFFT, GA ;

ERICKSON, J .

SCIENCE, 1990, 247 (4945) :954-958

[9] A SYNTHETIC HIV-1 PROTEASE INHIBITOR WITH ANTIVIRAL ACTIVITY ARRESTS HIV-LIKE PARTICLE MATURATION [J].

MCQUADE, TJ ;

TOMASSELLI, AG ;

LIU, L ;

KARACOSTAS, V ;

MOSS, B ;

SAWYER, TK ;

HEINRIKSON, RL ;

TARPLEY, WG .

SCIENCE, 1990, 247 (4941) :454-456

[10] PEPTIDE-SUBSTRATES AND INHIBITORS OF THE HIV-1 PROTEASE [J].

MOORE, ML ;

BRYAN, WM ;

FAKHOURY, SA ;

MAGAARD, VW ;

HUFFMAN, WF ;

DAYTON, BD ;

MEEK, TD ;

HYLAND, L ;

DREYER, GB ;

METCALF, BW ;

STRICKLER, JE ;

GORNIAK, JG ;

DEBOUCK, C .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 159 (02) :420-425

← 1 2 →