Kumar Pradeep, Narasimhan Balasubramanian, Ramasamy Kalavathy, Mani Vasudevan, Mishra Rakesh Kumar, Majeed Abu Bakar Abdul
Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak-124001, India.
Curr Top Med Chem. 2015;15(11):1050-64. doi: 10.2174/156802661511150408111252.
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 (pMICam = 1.67 μM/ml) was the most potent antimicrobial agent. The synthesized benzohydrazides were also having good anticancer potential and compound 22 (IC50 = 1.20 μM μM) 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 μM). 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)χ(v)) and Wiener index (W).
合成了一系列3/4-溴-N'-(取代亚苄基/呋喃-2-基亚甲基/5-氧代戊叉基/3-苯基烯丙叉基)苯甲酰肼(1-23)，并通过物理化学和光谱手段对其进行了表征。对合成的化合物进行了抗菌和抗癌潜力筛选。抗菌活性结果表明，化合物12(pMICam = 1.67 μM/ml)是最有效的抗菌剂。合成的苯甲酰肼也具有良好的抗癌潜力，发现化合物22(IC50 = 1.20 μM)是最有效的抗癌剂，其效力比标准药物粉防己碱(IC50 = 1.53)和5-氟尿嘧啶(IC50 = 4.6 μM)更强。定量构效关系研究表明，合成化合物的抗菌活性可用电子参数总能量(Te)、拓扑参数价零阶分子连接性指数((0)χ(v))和维纳指数(W)来最好地描述。
