Synthesis and Antifungal Activity of New Dihydropyrazoles of Designed Curcumin Analogues

V. Tripathi, N. Saxena
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引用次数: 1

Abstract

A library of new dihydropyrazole derivatives have been synthesized from well designed curcumin analogues by reaction of chalcone derivatives with phenylhydrazine. All the synthesized compounds were characterized by spectroscopic (1H and 13C NMR, IR spectra), spectrometric (Mass spectra) data and elemental analysis. Dihydro-pyrazoles exhibited characteristic dd (double doublet) due to presence of optically active carbon of pyrazole ring. All the synthesized compounds were also evaluated for their antifungal potential against six different fungal starins. Evaluated heterocyles showed potent inhibitory property against tested fungal strains with minimum inhibitory concentration (MIC) values upto 3.12 μg/mL. Heterocyles with nitro and methoxy substitutions were showing best antifungal activities. Among 20 different derivatives tested for biological activity SAR has been developed between the various substitutions at phenyl ring of synthesized heterocycles.
新型姜黄素类似物双氢吡唑的合成及抗真菌活性研究
以姜黄素类似物为原料,通过查尔酮衍生物与苯肼的反应,合成了一系列新的二氢吡唑衍生物。所有合成的化合物都通过波谱(1H和13C NMR, IR),光谱(质谱)数据和元素分析进行了表征。双氢吡唑类化合物由于存在吡唑环上的光学活性碳而表现出双双重态特征。所有合成的化合物还对六种不同的真菌起始物进行了抑菌活性评价。经鉴定的杂环化合物对真菌具有较强的抑制作用,最小抑制浓度(MIC)可达3.12 μg/mL。硝基和甲氧基取代杂环具有较好的抑菌活性。在20种不同的生物活性衍生物中,合成的杂环上苯基环的不同取代之间形成了SAR。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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