磺胺类药物的合成、光谱评价及药理筛选

A. Rehman, M. Abbasi, S. Z. Siddiqui, S. Rasool, Sadia Jabeen, Amar Joyia, A. S. Gondal
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引用次数: 1

摘要

磺胺类化合物被认为具有生物活性,是一类重要的药物化合物。它们构成了一类重要的抗菌剂、降糖剂、抗癌剂和利尿剂。这是世界上最早的化疗药物,但它们迅速产生的耐药性减少了它们的使用。本文以10% Na2CO3水溶液为反应介质,以取代苯胺(1a-c)和四氢呋喃-2-基甲基甲烷胺(1d)与取代苯磺酰氯(2a-d)为原料,合成了N-(2/4-取代苯基)-4-(取代)苯磺酰胺(3a-d)和N-(四氢呋喃-2-基甲基)-4-甲基苯磺酰胺(3e)。第二步,以氢化锂为活化剂,以N,N-二甲基甲酰胺(DMF)为反应介质,使合成的分子3a-e与不同的烷基/芳烷基卤化物(4a-j)反应,合成目标N-取代化合物5a-z,aa,bb。通过1H-NMR、IR、EI-MS等光谱技术对合成的化合物进行了表征;并进一步检测其抗菌活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, spectral evaluation and pharmacological screening of some sulfa drugs
Sulfonamides are considered to be biologically active and an important class of pharmaceutical compounds. These constitute an important class of antimicrobials, antidiabetics, anticancer and diuretics. These were the first chemotherapeutic drugs introduced to the world but their rapidly developed resistance decreased their use. In the present work, N-(2/4-substitutedphenyl)-4-(substituted)benzenesulfonamide (3a-d) and N-(tetrahydrofuran-2-ylmethyl)-4-methylbenzenesulfonamide (3e) were synthesized by the reaction of substituted aniline (1a-c) and tetrahydrofuran-2-ylmethanamine (1d) with substituted benzenesulfonyl chloride (2a-d) using 10% aqueous Na2CO3 solution as a reaction medium. In the second step, the synthesized molecules 3a-e were allowed to react different alkyl/aralkyl halides (4a-j) to synthesize the target N-substituted compounds, 5a-z,aa,bb, using lithium hydride as an activator and N,N-dimethylformamide (DMF) as a reaction medium. All the synthesized compounds were characterized by using spectral techniques such as 1H-NMR, IR and EI-MS; and further examined for their anti-bacterial activities.
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