Novel synthetic analogs of the Pseudomonas autoinducer

被引：73

作者：

Kline, T ^{[1
]}

Bowman, J

Iglewski, BH

de Kievit, T

Kakai, Y

Passador, L

机构：

[1] PathoGenesis Corp, Seattle, WA 98119 USA

[2] Univ Rochester, Dept Microbiol & Immunol, Rochester, NY 14642 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(99)00626-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Release of virulence factors in Pseudomonas aeruginosa is regulated by two N-acylhomoserine lactones, PAI-I and PAI-2, that activate the respective transcription factors LasR and RhlR. With the goal of developing novel therapeutic agents, we synthesized constrained analogs of PAI-I and evaluated them in P. aeruginosa, Two of the novel analogs bound to LasR and showed agonist activity in LasR stimulation of a lasI-lacZ reporter construct. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：3447 / 3452

页数：6

相关论文

共 29 条

[1]

Balcht A.L., 1994, PSEUDOMONAS AERUGINO, P73

[2] A new rational hypothesis for the pharmacophore of the active metabolite of leflunomide, a potent immunosuppressive drug [J].

Bertolini, G ;

Aquino, M ;

Biffi, M ;

dAtri, G ;

DiPierro, F ;

Ferrario, F ;

Mascagni, P ;

Somenzi, F ;

Zaliani, A ;

Leoni, F .

JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (13) :2011-2016

[3] THE CHEMISTRY OF PSEUDOMONIC ACID .14. SYNTHESIS AND IN-VIVO BIOLOGICAL-ACTIVITY OF HETEROCYCLYL SUBSTITUTED OXAZOLE DERIVATIVES [J].

BROOM, NJP ;

ELDER, JS ;

HANNAN, PCT ;

PONS, JE ;

OHANLON, PJ ;

WALKER, G ;

WILSON, J ;

WOODALL, P .

JOURNAL OF ANTIBIOTICS, 1995, 48 (11) :1336-1344

[4] AUTOREGULATION OF CARBAPENEM BIOSYNTHESIS IN ERWINIA-CAROTOVORA BY ANALOGS OF N-(3-OXOHEXANOYL)-L-HOMOSERINE LACTONE [J].

CHHABRA, SR ;

STEAD, P ;

BAINTON, NJ ;

SALMOND, GPC ;

STEWART, GSAB ;

WILLIAMS, P ;

BYCROFT, BW .

JOURNAL OF ANTIBIOTICS, 1993, 46 (03) :441-454

[5]

DAVIES DG, 1998, Patent No. 57618

[6] NITRONE CYCLO-ADDITIONS - AN EFFICIENT METHOD FOR THE HOMOLOGATION OF ALDEHYDES TO ALPHA,BETA-UNSATURATED ALDEHYDES [J].

DESHONG, P ;

LEGINUS, JM .

JOURNAL OF ORGANIC CHEMISTRY, 1984, 49 (18) :3421-3423

[7] READILY ACCESSIBLE 12-I-5 OXIDANT FOR THE CONVERSION OF PRIMARY AND SECONDARY ALCOHOLS TO ALDEHYDES AND KETONES [J].

DESS, DB ;

MARTIN, JC .

JOURNAL OF ORGANIC CHEMISTRY, 1983, 48 (22) :4155-4156

[8] ANALOGS OF THE AUTOINDUCER OF BIOLUMINESCENCE IN VIBRIO-FISCHERI [J].

EBERHARD, A ;

WIDRIG, CA ;

MCBATH, P ;

SCHINELLER, JB .

ARCHIVES OF MICROBIOLOGY, 1986, 146 (01) :35-40

[9] Quorum sensing: A novel target for anti-infective therapy [J].

Finch, RG ;

Pritchard, DI ;

Bycroft, BW ;

Williams, P ;

Stewart, GSAB .

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 1998, 42 (05) :569-571

[10] CLONING AND CHARACTERIZATION OF THE PSEUDOMONAS-AERUGINOSA LASR GENE, A TRANSCRIPTIONAL ACTIVATOR OF ELASTASE EXPRESSION [J].

GAMBELLO, MJ ;

IGLEWSKI, BH .

JOURNAL OF BACTERIOLOGY, 1991, 173 (09) :3000-3009