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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >Synthesis, characterization and biological evaluation of pyrazolones containing multi substituted thiazolidinones and oxadizoles
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Synthesis, characterization and biological evaluation of pyrazolones containing multi substituted thiazolidinones and oxadizoles

机译：含多取代噻唑烷酮和恶二唑的吡唑啉酮的合成，表征和生物学评价

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A series of novel Pyrazolone Schiff bases bearing thiazolidinone and oxadiazoles systems were prepared from ethyl- 2-(4-formyl-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)acetate (4) and substituted amines. All pyrazolone schiff bases were refluxed with mercapto acetic acid in presence of anhydrous zinc chloride and solvent N,N-dimethyl formamide to afforded novel series of Ethyl-2-(4-(3-(4-substitutedphenyl)-4-oxothiazolidin-2-yl)-3-methyl-5-oxo- 4,5-dihydro-1H-pyrazol-1-yl)acetate [5a-f]. Novel moieties 2-(1-((4-acetyl-5-(4-substituted phenyl)-5-methyl-4,5- dihydro-1,3,4-oxadiazol-2-yl) methyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)-3-(4-substituted phenyl) thiazolidin-4-one were synthesized by the condensation of (E)-2-(4-(3-(4-substitutedphenyl)-4-oxothiazolidin-2-yl)- 3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)-N'-(1-(4-substitutedphenyl)ethylidene)acetohydrazide (6a-f) and substituted ketones (7a-e) afford corresponding (E)-2-(4-(3-(4-substitutedphenyl)-4-oxothiazolidin-2-yl)-3-methyl-5- oxo-4,5-dihydro-1H-pyrazol-1-yl)-N'-(1-(4-substitutedphenyl) ethylidene)acetohydrazide (8a-f). This was subjected to cyclization with excess of acetic anhydride to give corresponding congeners 2-(1-((4-acetyl-5-(4- substitutedphenyl)-5-methyl-4,5-dihydro-1,3,4-oxadiazol-2-yl)methyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4- yl)-3-(4-substitutedphenyl) thiazolidin-4-one (9a-j) in excellent yields. The structures of these newly synthesized compounds were characterized by 1H-NMR, 13C-NMR, Mass, IR and elemental analysis. The prepared compounds have been screened on some strains of bacteria and fungi.
机译：用2-（4-甲酰基-3-甲基-5-氧代-4,5-二氢-1H-吡唑-1-基）乙酸乙酯制备一系列带有噻唑烷酮和恶二唑系统的新型吡唑啉酮席夫碱（4）和取代的胺。在无水氯化锌和溶剂N，N-二甲基甲酰胺的存在下，将所有吡唑啉酮席夫碱与巯基乙酸回流，得到新的乙基-2-（4-（3-（4-（4-取代苯基）-4-氧噻唑烷-2） -（基）-3-甲基-5-氧-4,5,2-二氢-1H-吡唑-1-基）乙酸酯[5a-f]。新的2-（1-（（4-乙酰基-5-（4-取代的苯基）-5-甲基-4,5-二氢-1,3,4-恶二唑-2-基）甲基）-3-甲基通过（E）-2-（4-（3）的缩合反应合成了-5-氧代-4,5-二氢-1H-吡唑-4-基）-3-（4-取代的苯基）噻唑烷-4- -（4-取代苯基）-4-氧噻唑烷-2-基）-3-甲基-5-氧代-4,5-二氢-1H-吡唑-1-基）-N'-（1-（4-取代苯基）亚乙基）乙酰肼（6a-f）和取代的酮（7a-e）得到相应的（E）-2-（4-（3-（4-取代苯基）-4-氧噻唑烷-2-基）-3-甲基-5 -氧代-4，5-二氢-1H-吡唑-1-基）-N′-（1-（4-取代的苯基）亚乙基）乙酰肼（8a-f）。将其与过量的乙酸酐进行环化，得到相应的同类物2-（1-（（4-乙酰基-5-（4-取代苯基）-5-甲基-4,5-二氢-1,3,4-恶二唑） -2-基）甲基）-3-甲基-5-氧代-4,5-二氢-1H-吡唑-4-基）-3-（4-取代苯基）噻唑烷-4-（9a-j）产量。这些新合成的化合物的结构通过1 H-NMR，13 C-NMR，质量，IR和元素分析进行​​了表征。在某些细菌和真菌菌株上筛选了制备的化合物。

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