Synthesis and in vitro antimicrobial activities of 2-hydroxy-6-methyl-7-(arylamino)-1,7-dihydropurin-8-ones

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• 作者：Sharma ; Pratibha ; Sharma ; Shikha ; Rane ; Nilesh
• 关键词：2-Hydroxy-6-methyl-7-(arylamino)-1 ; 7-dihydropurin-8-ones ; Molecular refractive index parameters (M_R) ; Hammett substituent constant (&#963 ; )
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2004
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：June 15, 2004
• 卷：12
• 期：12
• 页码：3135-3139
• 文件大小：266 K

摘要

A number of 2-hydroxy-6-methyl-7-(arylamino)-1,7-dihydropurin-8-ones have been synthesized. 3-Oxo-2-(arylhydrazono)butyric acid ethyl ester were acetylated and treated with triethyl amine and formamide in presence of 1,4-dioxane to yield N-(5-acetyl-4-ethoxy-2-oxo-2,5-dihydro-imidazol-1-yl)-N-arylacetamide, which on refluxation with urea and freshly prepared sodium ethoxide yielded the title compound. All the newly synthesized compounds have been characterized by spectroscopic and elemental analysis data. The synthesized compounds were screened against a representative panel of susceptible and resistant Gram-positive and Gram-negative bacteria using a standard antibiotic drug purinthol as control. Quantitative structure–activity relationship has also been interpreted in terms of correlation of biological activity with molecular refractive index parameters (M_R) and Hammett substituent constant (σ).