Synthesis and biological evaluation of a novel series of 2,2-bisaminomethylated aurone analogues as anti-inflammatory and antimicrobial agents

被引：94

作者：

Bandgar, Babasaheb R. ^{[1
,2
]}

Patil, Sachin A. ^{[1
]}

Korbad, Balaji L. ^{[1
]}

Biradar, Satish C. ^{[1
]}

Nile, Shivraj N. ^{[3
]}

Khobragade, Chandrahasya N. ^{[3
]}

机构：

[1] Swami Ramanand Teerth Marathwada Univ, Organ Chem Res Lab, Sch Chem Sci, Nanded 431606, MS, India

[2] Solapur Univ, Organ Chem Res Lab, Sch Chem Sci, Solapur 413255, MS, India

[3] Swami Ramanand Teerth Marathwada Univ, Biochem Res Lab, Sch Life Sci, Nanded 431606, MS, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 07期

关键词：

2,2-Bisaminomethylated aurones; Anti-inflammatory activity; Antimicrobial activity; TUMOR-NECROSIS-FACTOR; ANTIBACTERIAL ACTIVITY; FACTOR-ALPHA; LYMPHOTOXIN; INHIBITORS; EXPRESSION; RECEPTORS; FLAVONES;

D O I：

10.1016/j.ejmech.2010.03.045

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This is the first report on aurones as a new class of drugs with anti-inflammatory and antimicrobial agents. A series of 2,2-bisaminomethylated aurone analogues (4a-j) were synthesized by Mannich reaction from 1,3,5-trimethoxybenzene in three steps. The structures of the newly synthesized compounds were confirmed by IR, H-1 NMR and mass spectral analysis. All the synthesized compounds were screened against the pro-inflammatory cytokines (TNF-alpha, IL-6) and antimicrobial (antibacterial and antifungal) activity. Compounds 4a, 4b, 4c, 4d, and 4e showed promising results against IL-6 at 10 mu M concentration (74-100%). Compounds 4a, 4b and 4c were found to be active against TNF-alpha (76-100%) at 10 mu M. Interestingly, all compounds have shown good antimicrobial activity. Compounds 4d, 4e and 4f showed excellent antimicrobial activity as compared with standard drugs. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：3223 / 3227

页数：5

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