Synthesis of newer 1,2,3-triazole linked chalcone and flavone hybrid compounds and evaluation of their antimicrobial and cytotoxic activities

被引：171

作者：

Kant, Rama ^{[1
]}

Kumar, Dharmendra ^{[2
]}

Agarwal, Drishti ^{[3
]}

Gupta, Rinkoo Devi ^{[3
]}

Tilak, Ragini ^{[2
]}

Awasthi, Satish Kumar ^{[4
]}

Agarwal, Alka ^{[1
]}

机构：

[1] Banaras Hindu Univ, Inst Med Sci, Dept Med Chem, Varanasi 221005, Uttar Pradesh, India

[2] Banaras Hindu Univ, Inst Med Sci, Dept Microbiol, Varanasi 221005, Uttar Pradesh, India

[3] South Asian Univ, Fac Life Sci & Biotechnol, Delhi 110021, India

[4] Univ Delhi, Dept Chem, Chem Biol Res Lab, Delhi 110007, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 113卷

关键词：

1,2,3-Triazole; Chalcone; Antibacterial activity; Antifungal activity; Antiplasmodial activity; Cytotoxicity; ANTIPROLIFERATIVE ACTIVITY; BIOLOGICAL EVALUATION; DESIGN; ANTIMALARIAL; DERIVATIVES; SCAFFOLD;

D O I：

10.1016/j.ejmech.2016.02.041

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present study was carried out in an attempt to synthesize a new class of antimicrobial and anti-plasmodial agents by copper catalyzed click chemistry to afford 25 compounds 10-14(a-e) of 1,4-disubstituted-1,2,3-triazole derivatives of chalcones and flavones. The structures of the newly synthesized compounds were established by elemental analysis, IR, H-1 NMR, C-13 NMR and Mass spectral data. The newly synthesized compounds were evaluated for their antibacterial activity against Gram positive bacteria (Staphylococcus aureus, Enterococcus faecalis), Gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Shigella boydii, Klebsiella pneumoniae) and antifungal activity against (Candida albicans, Candida tropicalis, Candida parapsilosis, Cryptococcus neoformans, Dermatophyte) as well as molds (Aspergillus niger, Aspergillus fumigatus). The antiplasmodial and cytotoxic activities of these compounds were also evaluated against human malaria parasite Plasmodium falciparum strain 3D7 and human hepato-cellular carcinoma cells (Huh-7), respectively. Compounds 10a, 10c, 10d, 12c and 14e showed promising antibacterial activity while compounds 10e, 11d, 11e, 12c, 13a, 13b, 13e, 14a and 14d showed good antifungal activity as compared to the corresponding standard drugs. Compound 10b was found to be the most active against Plasmodium falciparum while the remaining compounds showed moderate to weak antiplasmodial activity. However, cytotoxic activities of all compounds were found ineffective against Huh-7 cells. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：34 / 49

页数：16

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