Microwave Assisted Synthesis, Characterization and Antimicrobial Screening of Thiazolidin-4-one Substituted Pyrazole Derivatives

IF 0.9 Q4 CHEMISTRY, MULTIDISCIPLINARY Current Microwave Chemistry Pub Date : 2019-10-24 DOI:10.2174/2213335606666190722144956
M. Beniwal, N. Jain
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引用次数: 3

Abstract

This paper describes the synthesis of novel thiazolidin-4-one substituted pyrazole derivatives from the condensation reaction of hydrazide with acetophenone derivatives. Herein we describe the synthesis of fourteen compounds by microwave irradiation method. The synthesized compounds are in excellent yield by utilizing microwave irradiation heating. Compounds using different aromatic or heteroaromatic compounds should be synthesized and screened for their antibacterial activity to explore the possibility of pyrazole substituted thiazolidin- 4-ones as a novel series of antimicrobials. Synthesis of thiazolidin-4-one substituted pyrazole derivatives was carried out under microwave radiation. These compounds were identified on the basis of melting point range, Rf values, IR, 1HNMR and mass spectral analysis. These compounds were evaluated for their in vitro antimicrobial activity and their Minimum Inhibitory Concentration (MIC) was determined. Among them Comp. 4b and Comp. 4k possess appreciable antimicrobial and antifungal activities. A novel series of Thiazolidin-4-one substituted pyrazole were synthesized under microwave irradiation method and identified on the basis of melting point range, Rf values, IR, 1HNMR, mass spectral data and elemental analysis. The compounds were subjected to in vitro antimicrobial screening and their Minimum Inhibitory Concentrations (MIC) were determined. Among all the tested compounds, two compounds 4b and 4k exhibited moderate to significant activity against all the tested strains of bacteria and fungus were found to have appreciable antimicrobial activities. The results of antibacterial activity showed that compounds containing electron withdrawing groups were found to be more active than the compounds containing electron releasing groups.
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噻唑烷-4- 1取代吡唑衍生物的微波合成、表征及抗菌筛选
本文介绍了由酰肼与苯乙酮衍生物的缩合反应合成新的噻唑烷-4-酮取代吡唑衍生物。本文用微波辐射法合成了14个化合物。利用微波辐射加热合成的化合物具有优异的产率。为了探索吡唑取代噻唑烷-4-酮作为一系列新型抗菌药物的可能性,应合成并筛选不同芳香族或杂芳香族化合物的化合物。在微波辐射下合成噻唑烷-4-酮取代吡唑衍生物。根据熔点范围、Rf值、IR、1HNMRand质谱分析对这些化合物进行了鉴定。对这些化合物的体外抗菌活性进行了评价,并测定了它们的最低抑菌浓度(MIC)。其中Comp。4band Comp。4k具有明显的抗菌和抗真菌活性。采用微波法合成了一系列新的噻唑烷-4-酮取代吡唑,并通过熔点范围、Rf值、IR、1HNMR、质谱数据和元素分析对其进行了鉴定。对化合物进行体外抗菌筛选,并测定其最小抑菌浓度(MIC)。在所有测试的化合物中,两个化合物4b和4k对测试的细菌和真菌菌株表现出中等至显著的抗菌活性。抗菌活性的结果表明,含有吸电子基团的化合物比含有电子释放基团的化合物更具活性。
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来源期刊
Current Microwave Chemistry
Current Microwave Chemistry CHEMISTRY, MULTIDISCIPLINARY-
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