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Design and Synthesis of 5-Oxoimidazolidine Derivatives in Search of Potent Antitubercular and Antifungal agents
被引:0
|作者:
Singirisetty, Triveni
[1
]
Chilamakuru, Naresh Babu
[2
]
Peraman, Ramalingam
[2
]
Mallela, Vijaya Jyothi
[1
]
Sana, Maheswari
[1
]
Begum, P. Inthiyaz
[3
]
机构:
[1] Raghavendra Inst Pharmaceut Educ & Res, Dept Pharmaceut Chem, Ananthapuramu, Andhra Pradesh, India
[2] Raghavendra Inst Pharmaceut Educ & Res, RERDS CPR, Mol Modeling & Drug Discovery Div, Ananthapuramu, Andhra Pradesh, India
[3] Raghavendra Inst Pharmaceut Educ & Res RIPER, Dept Pharmaceut Qual Assurance, Ananthapuramu, Andhra Pradesh, India
关键词:
Molecular docking;
ADMET studies;
5-Oxoimidazolidines;
Antitubercular activity;
Antifungal activity;
D O I:
暂无
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
5-Oxoimidazolidines are significant outfits because of their impending biological activity and also because of their resourcefulness as synthons in organic revolutions. The designed library was docked against the crystal structure of Mycobacterium tuberculosis enoyl reductase (2B35) and crystal structure of flavohemoglobin (3OZU) to know the best fit molecule. The ADMET parameters revealed that the compounds have synthetic acceptability and leadlikeness. Accordingly, the selected 5-oxoimidazolidines (S1-8 and A(1-8)) were synthesized from carbohydrazides (1a-h) and characterized by spectral data. Further, these compounds were screened against M tuberculosis H37RV by microplate Alamar Blue assay method. The compound S-3 showed minimum inhibitory concentration at 6.25 mu g/mL, while the antifungal screening demonstrated S-1 as a promising lead with the corresponding zone of inhibitions of 22 mm and 18 mm against Aspergillus niger and Candida albicans.
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页码:441 / 451
页数:11
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