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Click synthesis, antimicrobial, DNA photocleavage and computational studies of oxindole-tethered 1H-1,2,3-triazoles
被引:8
|作者:
Kumar, Vijay
[1
]
Lal, Kashmiri
[1
]
Kumar, Ravinder
[2
]
Kumar, Anil
[2
]
Mathpati, Ramling S.
[3
]
Singh, Madhur Babu
[4
]
Kumari, Kamlesh
[5
]
机构:
[1] Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India
[2] Guru Jambheshwar Univ Sci & Technol, Dept Bio & Nano Technol, Hisar 125001, Haryana, India
[3] Natl Inst Technol, Dept Chem, Kurukshetra 136119, Haryana, India
[4] Univ Delhi, Atma Ram Sanatan Dharma Coll, Dept Chem, New Delhi 110021, India
[5] Univ Delhi, Dept Zool, Delhi 110007, India
关键词:
antimicrobial;
click chemistry;
DNA photocleavage;
docking;
1;
2;
3-triazole;
oxindole;
x-ray diffraction;
CYCLOADDITION EN-ROUTE;
ANTIBACTERIAL;
UPDATE;
ISATIN;
DERIVATIVES;
ANTIFUNGAL;
CHEMISTRY;
DOCKING;
DESIGN;
ACID;
D O I:
10.4155/fmc-2023-0075
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
Aim: To obtain new hybrids derived from isatin and triazole. Materials & methods: A series of oxindole-1-H-1,2,3-triazole hybrids (4a-l) were synthesized from 3-sulfenylated N-propargylated oxindoles and organic azides employing Cu(I)-catalyzed azide-alkyne cycloaddition. These compounds were evaluated in vitro for antimicrobial activity by the standard serial dilution method and DNA photocleavage activity. Results: Antimicrobial assay revealed that compounds 4l and 4f exhibited promising efficacy against Candida albicans and Rhizopus oryzae, respectively, with a minimum inhibitory concentration (MIC) value of 0.0008 & mu;mol/mL. Compounds 4h and 4k completely degraded plasmid DNA. Further molecular docking of compounds with 1KZN (4j and 4k) and 5TZ1 (4h and 4l) revealed good binding interactions. Conclusion: Results of the current research can help in the development of new antimicrobial agents with high efficacy.
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页码:1115 / 1131
页数:17
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