新型吡唑并吡啶及吡唑并吡啶衍生物的合成、表征及抗菌活性评价

Savita R. Shejale, C. Rajput, Shubhangi S. Bansode, M. Kondawar
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引用次数: 2

摘要

为了满足抗菌、镇痛和抗真菌药物的结构要求,设计了一系列新的取代吡唑吡啶和吡唑吡啶,它们具有广泛的生物活性,如镇痛、抗菌、抗真菌等。(1)这些环的治疗重要性促使我们开发选择性分子。分别由1-苯基-3-(取代苯基)- 1h -吡唑-4-基}-3-苯基-1-丙烯-3-酮(查尔酮)(Vilsmeier-Haack反应)(2a-c)通过claisen schmidt反应制备1-{1-苯基-3-(取代苯基)- 1h -吡唑-4-甲醛(2 -c)。1-{1-苯基-3-(取代苯基)- 1h -吡唑-4-基}-3-苯基-1-丙烯-3- 1(查尔酮)(3a-c)进一步与硫脲、3-氨基-s-三唑、氰乙酸乙酯、cynothioacetamidea处理,得到1,2,3,4四氢嘧啶(4a -c)、三唑嘧啶(5a,b)、cynophenylpyridine(6a -c)和苯基吡啶硫酮衍生物。对新合成的化合物进行了结构表征,并对其抑菌活性进行了研究。参考以阿莫西林为标准药物,用圆盘扩散法测定化合物4a、4c、5a、6c、7c对枯草芽孢杆菌、金黄色葡萄球菌、寻常变形杆菌的抑菌活性,结果表明化合物4a、4c、5a、6c、7c具有较高的抑菌活性。和假单胞菌。相似的化合物4c和7c对白色念珠菌的抑菌活性最大
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, characterisation, evaluation of antimicrobial & antifungal activity of novel pyrazolopyrimidine & pyrazolopyridine derivatives
A new series of substituted PyrazoloPyrimidine & Pyrazolopyridine were designed to meet the structural requirement of antimicrobial ,Analgesic & antifungal drugs which has been known to possess a broad spectrum of biological activities such as analgesic,antimicrobial antifungal etc .(1) The therapeutic importance of these rings prompted us to develop selective molecules. The starting material of 1-{1-phenyl-3-(substituted phenyl)-1H-pyrazol-4-yl}-3-phenyl-1-propen-3-one (Chalcone) (3a-c) prepared from by claisen schmidt reaction from respective 1-phenyl-3-(substituted phenyl)-1H-pyrazoles-4-carboxaldehyde (Vilsmeier-Haack Reaction) ( 2a-c). 1-{1-phenyl-3-(substituted phenyl)-1H-pyrazol-4-yl}-3-phenyl-1-propen-3-one (Chalcone) (3a-c) further treated with thiourea ,3amino-s-triazole,ethylcyanoacetate, cynothioacetamideto produced 1,2,3,4 tetrahydropyrimidine (4 a-c),triazolopyrimidine (5 a,b),cynophenylpyridine(6 a-c) & phenyl pyridine thione derivatives.The structures of newly Synthesised compounds were characterized by spectral data & studied for their antimicrobial & Antifungal activities. Compounds 4a, 4c, 5a, 6c, 7c showed high antimicrobial activity using disc diffusion method with reference to using Amoxicillin as standard drug active active against Bacillus substillus, staphylococcus aureus, Proteus vulgaris.and pseudomonas.Similary compound 4c&7c showed maximum antifungal activity against fungal species candida albicans
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