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:38
|
作者
Sindhu, Jayant [1 ]
Singh, Harjinder [1 ]
Khurana, J. M. [1 ]
Bhardwaj, Jitender Kumar [2 ]
Saraf, Priyanka [2 ]
Sharma, Chetan [3 ]
机构
[1] Univ Delhi, Dept Chem, Delhi 110007, India
[2] Kurukshetra Univ Kurukshetra, Dept Zool, Reprod Physiol Lab, Kurukshetra 136119, Haryana, India
[3] MMU, Dept Biotechnol, Mullana 133207, Haryana, India
关键词
Apoptosis; Ovarian follicles; One-pot; 1,2,3-triazoles; Pyrazole; Antimicrobial; Click chemistry; Multicomponent; Green; CLICK CHEMISTRY; DRUG DISCOVERY; CU-I; INHIBITORS; DERIVATIVES; ACID; 1,2,3-TRIAZOLES; ANTAGONISTS; RECEPTORS; PATHWAY;
D O I
10.1007/s00044-016-1604-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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 CuSO4.5H(2)O 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.
引用
收藏
页码:1813 / 1830
页数:18
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