辣木碱n -取代磺胺类脂氧合酶抑制剂的合成

M. Abbasi, U. Mujahid, Aziz‐ur‐Rehman, S. Rasool, K. Khan, M. Ashraf
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引用次数: 3

摘要

磺胺类药物是一类具有良好抑制作用的新兴药物。本文合成了一系列n -苄基-4-氯苯磺酰胺的n取代衍生物。辣木碱(苄胺)的反应;1)与4氯苯磺酰氯(2)在水溶液中生成母体分子n -苄基-4氯苯磺酰胺(3)。烷基/芳烷基卤化物(4a-m)与3在极性非质子介质中反应生成n取代衍生物(5a-m)。合成产物经核磁共振(H-NMR)、红外光谱(IR)和质谱(EI-MS)表征,并经脂氧合酶(LOX)筛选。这些被发现是这种酶的适度抑制剂,可以用作各种炎症性疾病的治疗剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of Some N-Substituted Sulfonamides Derived from Moringine as Lipoxygenase Inhibitors
Sulfonamides belong to an emerging class having good inhibitory effects. In the present work, a series of N-substituted derivatives of N-benzyl-4-chlorobenzenesulfonamide have been synthesized. The reaction of moringine (benzylamine; 1) with 4chlorobenzenesulfonyl chloride (2) in aqueous medium yielded the parent molecule, N-benzyl-4-chlorobenzenesulfonamide (3). Alkyl/aralkyl halides, 4a-m, were reacted with 3 in polar aprotic medium to produce N-substituted derivatives, 5a-m. These synthesized products were characterized by H-NMR, IR and EI-MS spectra and screened against lipoxygenase (LOX) enzyme. These were found to be moderate inhibitors of this enzyme and could find their use as therapeutic agent for various inflammatory ailments.
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