Design and synthesis of (3,5-disubstituted isoxazole)-linked [1,5]-benzodiazepine conjugates: evaluation of their antimicrobial and anti-tyrosinase activities

被引：5

作者：

Abdallah, Wejdane ^{[1
,2
]}

Daami-Remadi, Mejda ^{[3
]}

Znati, Mansour ^{[2
]}

Ben Jannet, Hichem ^{[2
]}

Gharbi, Rafik ^{[1
]}

机构：

[1] Univ Monastir, Fac Sci Monastir, Lab Appl Chem & Environm, Monastir 5019, Tunisia

[2] Univ Monastir, Lab Heterocycl Chem, Team Med Chem & Nat Prod & React, Fac Sci Monastirm,Nat Prod & React LR11SE39, Monastir 5019, Tunisia

[3] Sousse Univ, Integrated Hort Prod Tunisian Ctr East, Reg Ctr Res Hort & Organ Agr Chott Mariem, Chott Mariem 4042, Tunisia

来源：

JOURNAL OF CHEMICAL RESEARCH | 2017年 / 01期

关键词：

1,5-benzodiazepine; 1,5-benzodiazepine-2-thione; 3,5-disubstituted isoxazole; hybrid molecules; click chemistry; antimicrobial; antityrosinase; BIOLOGICAL EVALUATION; DERIVATIVES;

D O I：

10.3184/174751917X14815427219121

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of novel 2-(3,5-disubstituted isoxazolyl)-1,5-benzodiazepines and 2,4-bis-(3,5-disubstituted isoxazolyl)-1,5-benzodiazepine derivatives have been designed and synthesised by employing an alkyne/nitrile oxide cycloaddition 'click' type chemistry protocol. The structures of the compounds were determined on the basis of H-1, C-13 and 2D-NMR techniques and by HRMS analysis. These hybrid molecules exhibit moderate to significant antimicrobial and anti-tyrosinase activities.

引用

页码：12 / 17

页数：6

共 21 条

[1]

[Anonymous], 1987, BACTERIOLOGIE MEDICA

[2]

Barry A.L., 1991, MANUAL CLIN MICROBIO, P1117

[3] Neuropharmacological screening of two 1,5-benzodiazepine compounds in mice [J].