2-AZETIDINONE DERIVATIVES: SYNTHESIS, ANTIMICROBIAL, ANTICANCER EVALUATION AND QSAR STUDIES

被引：0

作者：

Deep, Aakash ^{[1
]}

Kumar, Pradeep ^{[1
]}

Narasimhan, Balasubramanian ^{[1
]}

Lim, Siong Meng ^{[2
,4
]}

Ramasamy, Kalavathy ^{[2
,4
]}

Mishra, Rakesh Kumar ^{[2
,3
]}

Mani, Vasudevan ^{[2
,3
]}

机构：

[1] Maharshi Dayanand Univ, Fac Pharmaceut Sci, Rohtak 124001, Haryana, India

[2] Univ Teknol MARA UiTM, Fac Pharm, Bandar Puncak Alam 42300, Selangor, Malaysia

[3] Univ Teknol MARA UiTM, Brain Degenerat & Therapeut Grp, Shah Alam 40450, Selangor Darul, Malaysia

[4] Univ Teknol MARA UiTM, Brain & Neurosci Commun Res, Collaborat Drug Discovery Res CDDR Grp, Shah Alam 40450, Selangor Darul, Malaysia

来源：

ACTA POLONIAE PHARMACEUTICA | 2016年 / 73卷 / 01期

关键词：

2-azetidinone; antimicrobial; anticancer; QSAR; ACID;

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A series of 2-azetidinone derivatives was synthesized from hippuric acid and evaluated for its in vivo antimicrobial and anticancer activities. Antimicrobial properties of the title compounds were investigated against Gram positive and Grant negative bacterial as well as fungal strains. Anticancer activity was performed against breast cancer (MCF7) cell lines. Antimicrobial activity results revealed that N-[2-[3-chloro-2-(2chloropheny1)-4-oxoazetidin- 1-ylamino1-2-oxoethyl ]benzamide (4) was found to be the most potent antimicrobial agent. Results of anticancer study indicated that the synthesized compounds exhibited average anticancer potential and N-[2-(3-chloro-2-oxo-4-styrylazeiidin-1-ylamino)-2-oxoethyltbenzamide(17) was found to be most potent anticancer agent against breast cancer (MCF7) cell lines. QSAR models indicated that the antibacterial, antifungal and the overall antimicrobial activities of the synthesized compounds were governed by topological parameters, Balaban index (1) and valence zero and first order molecular connectivity indices 'chi' and 'chi').

引用

页码：65 / 78

页数：14

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