Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif

P. N. Patel, Denish C. Karia
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Abstract

Novel series of diversely substituted acetyl pyrazoline having biphenyl carbonitrile motif have been synthesized. The reaction of 2-cyno-4’-bromomethyl biphenyl with1-(4-hydroxy-phenyl)-ethanone resulted in acetophenone derivative of biphenyl-2-carbonitrile. This acetophenone derivative was condensed with substituted aromatic aldehyde in mixed solvent resulted in various substituted chalcones. These chalcones were further cyclized using hydrazine hydrate in presence of glacial acetic acid to produce titled compound derivatives. The chemical structures of synthesized compounds were elucidated by 1H-NMR, 13C-NMR FT-IR and mass spectra. Synthesized compounds were screened for their antimicrobial activity by broth dilution method. Out of twelve newly synthesized compounds, eight compounds are found to be equipotent to Ampicillin.
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新型含联苯碳腈多取代乙酰吡唑啉基序的合成及抗菌活性研究
合成了一系列具有联苯碳腈基序的异取代乙酰吡唑啉。2-cyno-4′-溴甲基联苯与1-(4-羟基苯基)-乙酮反应,得到了2-联苯-碳腈的苯乙酮衍生物。该苯乙酮衍生物与取代芳醛在混合溶剂中缩合得到各种取代查尔酮。这些查尔酮在冰醋酸存在下用水合肼进一步环化,得到命名的化合物衍生物。通过1H-NMR、13C-NMR FT-IR和质谱对合成化合物的化学结构进行了表征。用肉汤稀释法对合成的化合物进行抑菌活性筛选。在12个新合成的化合物中,有8个化合物被发现与氨苄西林具有同等效力。
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