Synthesis and Antimicrobial Activity of Novel Heterocyclic Sulfamoyl-phenyl-carboximidamides Derived from Clinically Applied Sulfonamides
作者:Katarzyna Gobis、Henryk Foks、Katarzyna Wiśniewska、Maria Dąbrowska-Szponar、Ewa Augustynowicz-Kopeć、Agnieszka Napiórkowska
DOI:10.1002/ardp.201200160
日期:2012.11
A series of novel heterocyclic sulfamoyl‐phenyl‐carboximidamides were synthesized in satisfactory yields via condensation of clinically applied sulfonamides with heterocyclic methyl carbimidates. New structures were confirmed by IR and NMR spectra as well as elemental analyses. All the compounds were screened for their antibacterial, antifungal, and tuberculostatic activities. Preliminary results indicated
通过临床应用的磺酰胺与杂环甲基碳酰亚胺酯的缩合,合成了一系列新型杂环氨磺酰基-苯基-羧酰亚胺酰胺,收率令人满意。新结构通过 IR 和 NMR 光谱以及元素分析得到证实。筛选了所有化合物的抗菌、抗真菌和抗结核活性。初步结果表明,一些目标化合物表现出良好的抗菌效力。特别是,发现 N-[4-(噻唑-2-氨磺酰基)苯基]吡嗪-2-羧酰亚胺酰胺 (16) 与临床应用的磺胺甲氧哒嗪一样有效。