Synthesis and biological evaluation of some functionalized 1H-1,2,3-triazole tethered pyrazolo[3,4-b]pyridin-6(7H)-ones as antimicrobial and apoptosis inducing agents

被引:0
作者
Jayant Sindhu
Harjinder Singh
J. M. Khurana
Jitender Kumar Bhardwaj
Priyanka Saraf
Chetan Sharma
机构
[1] University of Delhi,Department of Chemistry
[2] Kurukshetra University Kurukshetra,Reproductive Physiology Laboratory, Department of Zoology
[3] MMU,Department of Biotechnology
来源
Medicinal Chemistry Research | 2016年 / 25卷
关键词
Apoptosis; Ovarian follicles; One-pot; 1,2,3-triazoles; Pyrazole; Antimicrobial; Click chemistry; Multicomponent; Green;
D O I
暂无
中图分类号
学科分类号
摘要
A series of novel molecular hybrids containing pyrazole, pyridinone and 1,2,3-triazoles have been synthesized by one-pot four-component reaction of Meldrum’s acid, substituted aryl azides, 4-(prop-2-yn-1-yloxy)aryl aldehyde and 3-methyl-1-phenyl-1H-pyrazol-5-amine using L-proline as a basic organocatalyst besides CuSO4.5H2O and sodium ascorbate as catalysts for click chemistry in PEG-400 as a highly efficient and green media. Apoptosis studies have been carried out on ovarian follicles of goat (Capra hircus) and in vitro antibacterial activity has been done against six strains namely Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa and antifungal activity against two yeast strains namely, Candida albicans and Saccharomyces cerevisiae.
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页码:1813 / 1830
页数:17
相关论文
共 209 条
[21]  
Bhardwaj JK(2005)The hallmarks of cancer Eur J Med Chem 74 2964-2974
[22]  
Saraf P(2003)Copper(I)-catalyzed synthesis of azoles. DFT study predicts unprecedented reactivity and intermediates Lancet Oncol 1 1677-1684
[23]  
Bhardwaj JK(2009)Synthesis, characterization and antimicrobial activity of some substituted 1,2,3-triazoles J Org Chem 14 1829-1852
[24]  
Saraf P(1998)Anticancer therapy targeting the apoptotic pathway J Chem Soc Perkin Trans 18 1468-1473
[25]  
Chandak N(2007)Peptide cyclization and cyclodimerization by cui-mediated azide−alkyne cycloaddition Curr Med Chem 8 1128-1137
[26]  
Bhardwaj JK(2008)Antitumour polycyclic acridines. Part 5.1 synthesis of 7H-pyrido[4,3,2- Bioorg Med Chem Lett 96 436-444
[27]  
Dimitrova DZ(2003) ]acridines with exploitable functionality in the pyridine ring Drug Discov Today 17 4297-4302
[28]  
Kitanov G(2015)Molecular hybridization: a useful tool in the design of new drug prototypes Eur J Med Chem 44 1522-1527
[29]  
Sharma RK(2007)Synthesis of 1,2,3-triazole-linked pyrrolobenzodiazepine conjugates employing ‘click’ chemistry: DNA-binding affinity and anticancer activity Bioorg Med Chem Lett 61 9118-9128
[30]  
Sharma PK(2008)The growing impact of click chemistry on drug discovery Russ J Org Chem 11 2529-2531