1,4-disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI)

被引：113

作者：

Heerding, DA ^{[1
]}

Chan, G ^{[1
]}

DeWolf, WE ^{[1
]}

Fosberry, AP ^{[1
]}

Janson, CA ^{[1
]}

Jaworski, DD ^{[1
]}

McManus, E ^{[1
]}

Miller, WH ^{[1
]}

Moore, TD ^{[1
]}

Payne, DJ ^{[1
]}

Qiu, XY ^{[1
]}

Rittenhouse, SF ^{[1
]}

Slater-Radosti, C ^{[1
]}

Smith, W ^{[1
]}

Takata, DT ^{[1
]}

Vaidya, KS ^{[1
]}

Yuan, CCK ^{[1
]}

Huffman, WF ^{[1
]}

机构：

[1] GlaxoSmithKlin Pharmaceut, Antibacterials & Host Def, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(01)00404-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1,4-Disubstituted imidazole inhibitors of Staphylococcus aureus and Escherichia coli enoyl acyl carrier protein reductase (FabI) have been identified. Crystal structure data shows the inhibitor 1 bound in the enzyme active site of E. coli FabI. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2061 / 2065

页数：5

共 18 条

[1]

ANTONINI I, 1983, SYNTHESIS-STUTTGART, P47

[2] BETA-1-SELECTIVE ADRENOCEPTOR ANTAGONISTS - EXAMPLES OF THE 2-[4-[3-(SUBSTITUTED AMINO)-2-HYDROXYPROPOXY]PHENYL]IMIDAZOLE CLASS .2. [J].

BALDWIN, JJ ;

CHRISTY, ME ;

DENNY, GH ;

HABECKER, CN ;

FREEDMAN, MB ;

LYLE, PA ;

PONTICELLO, GS ;

VARGA, SL ;

GROSS, DM ;

SWEET, CS .

JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (06) :1065-1080

[3] NONQUATERNARY CHOLINESTERASE REACTIVATORS .3. 3(5)-SUBSTITUTED 1,2,4-OXADIAZOL-5(3)-ALDOXIMES AND 1,2,4-OXADIAZOLE-5(3)-THIOCARBOHYDROXIMATES AS REACTIVATORS OF ORGANOPHOSPHONATE-INHIBITED EEL AND HUMAN ACETYLCHOLINESTERASE INVITRO [J].

BEDFORD, CD ;

HOWD, RA ;

DAILEY, OD ;

MILLER, A ;

NOLEN, HW ;

KENLEY, RA ;

KERN, JR ;

WINTERLE, JS .

JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (11) :2174-2183

[4] New directions in antibacterial research [J].

Chu, DTW ;

Plattner, JJ ;

Katz, L .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (20) :3853-3874

[5]

CLIFF MD, 1994, SYNTHESIS-STUTTGART, P681

[6] FATTY-ACID METABOLISM IN BACTERIA [J].

FULCO, AJ .

PROGRESS IN LIPID RESEARCH, 1983, 22 (02) :133-160

[7] ENOYL-ACYL CARRIER PROTEIN REDUCTASE (FABI) PLAYS A DETERMINANT ROLE IN COMPLETING CYCLES OF FATTY-ACID ELONGATION IN ESCHERICHIA-COLI [J].

HEATH, RJ ;

ROCK, CO .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1995, 270 (44) :26538-26542

[8] Mechanism of triclosan inhibition of bacterial fatty acid synthesis [J].

Heath, RJ ;

Rubin, JR ;

Holland, DR ;

Zhang, EL ;

Snow, ME ;

Rock, CO .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1999, 274 (16) :11110-11114

[9]

HORNE DA, 1994, HETEROCYCLES, V39, P139

[10]

Kawasaki I, 1998, HETEROCYCLES, V48, P1887

← 1 2 →