Synthesis, Antimicrobial, Anticancer Evaluation and QSAR Studies of 3/4-Bromo Benzohydrazide Derivatives

被引:16
作者
Kumar, Pradeep [1 ]
Narasimhan, Balasubramanian [1 ]
Ramasamy, Kalavathy [2 ]
Mani, Vasudevan [3 ]
Mishra, Rakesh Kumar [3 ]
Majeed, Abu Bakar Abdul [3 ]
机构
[1] Maharshi Dayanand Univ, Fac Pharmaceut Sci, Rohtak 124001, Haryana, India
[2] Univ Teknol MARA UiTM, Fac Pharm, Collaborat Drug Discovery Res Grp, Bandar Puncak Alam 42300, Selangor, Malaysia
[3] Univ Teknol MARA UiTM, Fac Pharm, Brain Res Lab, Bandar Puncak Alam 42300, Selangor, Malaysia
关键词
Anticancer activity; Antimicrobial activity; Benzohydrazides; Minimum bactericidal/fungicidal concentration; Minimum inhibitory concentration; QSAR studies; ANTIFUNGAL ACTIVITY; UNIFIED QSAR; PREDICTION; CHEMISTRY; HYDRAZIDES; COMPLEX; DESIGN; MODELS; ACIDS;
D O I
10.2174/156802661511150408111252
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series 3/4-bromo-N'-(substituted benzylidene/furan-2-ylmethylene/5-oxopentylidene/3-phenylallylidene)benzohydrazides (1-23) was synthesized and characterized by physicochemical and spectral means. The synthesized compounds were screened for their antimicrobial and anticancer potentials. Antimicrobial activity results indicated that compound 12 (pMIC(am) = 1.67 mu M/ml) was the most potent antimicrobial agent. The synthesized benzohydrazides were also having good anticancer potential and compound 22 (IC50 = 1.20 mu M mu M) was found to be the most potent anticancer agent which was more potent than standard drugs, tetrandrine (IC50 = 1.53) and 5-fluorouracil (IC50 = 4.6 mu M). QSAR studies indicated that antimicrobial activity of synthesized compounds was best described by electronic parameter, total energy (Te) and topological parameters, valance zero order molecular connectivity index ((0)chi(v)) and Wiener index (W).
引用
收藏
页码:1050 / 1064
页数:15
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