Design, Synthesis and Biological Evaluation of Some Novel Chalcone-Sulfonamide Hybrids

Mahammadali M. Khanusiya
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引用次数: 2

Abstract

A series of novel chalcone tethered sulphonamide hybrids 3a-5f were fabricated by condensing appropriate sulphonamide scaffold with methoxy and/or hydroxy substituted chalcones as a multi-target drug for therapeutic treatment. Chalcones were prepared by Claisen-Schmidt condensation of a substituted aldehyde with para aminoacetophenone. The synthesized chalconesulphonamide hybrids were screened by means of their antibacterial activity by NCCLS method. Among all these compounds, 5e and 5c were observed to displaying more potent growth inhibitory activity against bacterial strain and hybrid 5a shows more obvious antifungal activity. FT-IR, NMR and HR-LCMS spectral study assert the structures of synthesized sulphonamide chalcone hybrids.
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一些新型查尔酮-磺胺杂化物的设计、合成及生物学评价
通过适当的磺胺支架与甲氧基和/或羟基取代的查尔酮缩合,制备了一系列新型查尔酮系磺胺杂合体3a-5f,作为多靶点药物进行治疗。以取代醛和对氨基苯乙酮为原料,采用Claisen-Schmidt缩合法制备查尔酮。利用NCCLS法对合成的氯代磺酰胺杂合物进行抑菌活性筛选。其中,5e和5c对菌株的生长抑制活性更强,杂合物5a的抑菌活性更明显。FT-IR、NMR和HR-LCMS对合成的磺胺类查尔酮杂化物的结构进行了表征。
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