An Efficient Route to N-Monosubstituted Guanidino-Lactams

被引：2

作者：

Tommasi, Sara ^{[1
]}

Zanato, Chiara ^{[1
]}

Carabeo, Rey ^{[2
]}

Mangoni, Arduino A. ^{[3
,4
]}

Dall'Angelo, Sergio ^{[1
]}

Zanda, Matteo ^{[1
,5
]}

机构：

[1] Univ Aberdeen, Inst Med Sci, Kosterlitz Ctr Therapeut, Foresterhill AB25 2ZD, Scotland

[2] Univ Aberdeen, Inst Med Sci, Bacteriol Sect, Programme Microbiol, Foresterhill AB25 2ZD, Scotland

[3] Flinders Univ S Australia, Sch Med, Dept Clin Pharmacol, Bedford Pk, SA 5042, Australia

[4] Flinders Med Ctr, Bedford Pk, SA 5042, Australia

[5] CNR ICRM, I-20131 Milan, Italy

来源：

SYNTHESIS-STUTTGART | 2015年 / 47卷 / 19期

关键词：

guanidines; guanylation; lactams; cyclization; antimicrobials; PRO-ARG-H; THROMBIN INHIBITORS; ARGININE; DESIGN;

D O I：

10.1055/s-0034-1378845

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A small library of guanidino-lactams were synthesized in four steps and good overall yields by following the routes: preparation of guanylating agents, synthesis of protected guanidino-acids, cyclization to fully protected guanidino-lactams, and deprotection to the target compounds. The guanidino-lactams were assayed as antimicrobials on E. coli showing no significant antibiotic activity.

引用

页码：3067 / 3078

页数：12

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