环己酮是重要的化工原料,是生产尼龙6和尼龙66重要中间体,环己酮结构还存在于自然界中,是一类具有多种生物活性的药物骨架。本论文以双苄叉丙酮与丙二腈为原料,以DMF(N,N-二甲基甲酰胺)为溶剂,K_(2)CO_(3)为碱,且在无催化剂的条件下发生...环己酮是重要的化工原料,是生产尼龙6和尼龙66重要中间体,环己酮结构还存在于自然界中,是一类具有多种生物活性的药物骨架。本论文以双苄叉丙酮与丙二腈为原料,以DMF(N,N-二甲基甲酰胺)为溶剂,K_(2)CO_(3)为碱,且在无催化剂的条件下发生[5+1]环化反应,合成了一系列多取代环己酮类化合物,其结构经1 H NMR,^(13)C NMR、HR-MS(ESI)和IR表征,并对该合成反应机理进行了探讨。该合成方法具有宽泛的底物普适性,条件温和,较高的原子经济性和收率高等优势。展开更多
A series of indazol-2-yl(pyridin-4-yl)methanones, 4 were acquired from 2,6-bisbenzylidene cyclohex- anones, 3 and anti-tubercular drug (isoniazid), and their anti-tubercular impacts were screened. Among the test c...A series of indazol-2-yl(pyridin-4-yl)methanones, 4 were acquired from 2,6-bisbenzylidene cyclohex- anones, 3 and anti-tubercular drug (isoniazid), and their anti-tubercular impacts were screened. Among the test compounds used against Mycobacterium tuberculosis H37 Ra cell line in the microplate alamar blue assay, the compounds 4g-j revealed moderate anti-tubercular activity with MIC 12.5 μg/mL, comparable to standard drugs (streptomycin, MIC, 6.25 μg/mL, pyrazinamide, isoniazid and ciprofloxacin with MICs of 3.125 μg/mL).展开更多
文摘环己酮是重要的化工原料,是生产尼龙6和尼龙66重要中间体,环己酮结构还存在于自然界中,是一类具有多种生物活性的药物骨架。本论文以双苄叉丙酮与丙二腈为原料,以DMF(N,N-二甲基甲酰胺)为溶剂,K_(2)CO_(3)为碱,且在无催化剂的条件下发生[5+1]环化反应,合成了一系列多取代环己酮类化合物,其结构经1 H NMR,^(13)C NMR、HR-MS(ESI)和IR表征,并对该合成反应机理进行了探讨。该合成方法具有宽泛的底物普适性,条件温和,较高的原子经济性和收率高等优势。
基金VIT University for providing us with research funding and laboratory facilitiesMaratha Mandal Dental College,Belgaum for biological screening support
文摘A series of indazol-2-yl(pyridin-4-yl)methanones, 4 were acquired from 2,6-bisbenzylidene cyclohex- anones, 3 and anti-tubercular drug (isoniazid), and their anti-tubercular impacts were screened. Among the test compounds used against Mycobacterium tuberculosis H37 Ra cell line in the microplate alamar blue assay, the compounds 4g-j revealed moderate anti-tubercular activity with MIC 12.5 μg/mL, comparable to standard drugs (streptomycin, MIC, 6.25 μg/mL, pyrazinamide, isoniazid and ciprofloxacin with MICs of 3.125 μg/mL).