Structure-based design of non-peptide HIV protease inhibitors

被引：30

作者：

Ghosh, AK

Shin, D

Swanson, L

Krishnan, K

Cho, H

Hussain, KA

Walters, DE

Holland, L

Buthod, J

机构：

[1] Univ Illinois, Dept Chem, Chicago, IL 60607 USA

[2] Finch Univ Hlth Sci Chicago Med Sch, Dept Biol Chem, N Chicago, IL 60064 USA

[3] IT Res Inst, Dept Life Sci, Chicago, IL 60616 USA

来源：

FARMACO | 2001年 / 56卷 / 1-2期

关键词：

protease; inhibitor; ligand; design; non-peptide;

D O I：

10.1016/S0014-827X(01)01025-4

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A. number of structurally novel P-2-ligands have been designed and synthesized. Incorporation of these ligands in the (R)-(hydroxyethyl)sulfonamide isostere provided a series of potent non-peptidyl HIV protease inhibitors. (C) 2001 Elsevier Science S.A. All rights reserved.

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收藏

页码：29 / 32

页数：4

相关论文

共 13 条

[1] Recent developments in antiretroviral therapies [J].

Cihlar, T ;

Bischofberger, N .

ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 35, 2000, 35 :177-189

[2]

ERICKSONVITTANE.S, 1997, COMMUNICATION 1202

[3] HIV-protease inhibitors [J].

Flexner, C .

NEW ENGLAND JOURNAL OF MEDICINE, 1998, 338 (18) :1281-1292

[4] Structure based design:: Novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors [J].

Ghosh, AK ;

Krishnan, K ;

Walters, DE ;

Cho, WH ;

Cho, H ;

Koo, Y ;

Trevino, J ;

Holland, L ;

Buthod, J .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (08) :979-982

[5] Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere [J].

Ghosh, AK ;

Kincaid, JF ;

Cho, WH ;

Walters, DE ;

Krishnan, K ;

Hussain, KA ;

Koo, Y ;

Cho, H ;

Rudall, C ;

Holland, L ;

Buthod, J .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (06) :687-690

[6] Nonpeptidal P-2 ligands for HIV protease inhibitors: Structure-based design, synthesis, and biological evaluation [J].

Ghosh, AK ;

Kincaid, JF ;

Walters, DE ;

Chen, Y ;

Chaudhuri, NC ;

Thompson, WJ ;

Culberson, C ;

Fitzgerald, PMD ;

Lee, HY ;

McKee, SP ;

Munson, PM ;

Duong, TT ;

Darke, PL ;

Zugay, JA ;

Schleif, WA ;

Axel, MG ;

Lin, J ;

Huff, JR .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (17) :3278-3290

[7] CYCLIC SULFONE-3-CARBOXAMIDES AS NOVEL P-2-LIGANDS FOR RO-31-8959 BASED HIV-1 PROTEASE INHIBITORS [J].

GHOSH, AK ;

THOMPSON, WJ ;

MUNSON, PM ;

LIU, WM ;

HUFF, JR .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (01) :83-88

[8] 3-TETRAHYDROFURAN AND PYRAN URETHANES AS HIGH-AFFINITY P2-LIGANDS FOR HIV-1 PROTEASE INHIBITORS [J].

GHOSH, AK ;

THOMPSON, WJ ;

MCKEE, SP ;

DUONG, TT ;

LYLE, TA ;

CHEN, JC ;

DARKE, PL ;

ZUGAY, JA ;

EMINI, EA ;

SCHLEIF, WA ;

HUFF, JR ;

ANDERSON, PS .

JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (02) :292-294

[9] RECENT STUDIES OF THE ANOMERIC EFFECT [J].

JUARISTI, E ;

CUEVAS, G .

TETRAHEDRON, 1992, 48 (24) :5019-5087

[10] CRYSTAL-STRUCTURE OF HIV-1 PROTEASE IN COMPLEX WITH VX-478, A POTENT AND ORALLY BIOAVAILABLE INHIBITOR OF THE ENZYME [J].

KIM, EE ;

BAKER, CT ;

DWYER, MD ;

MURCKO, MA ;

RAO, BG ;

TUNG, RD ;

NAVIA, MA .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1995, 117 (03) :1181-1182