报告 - 合成有前景的抗菌剂和抗真菌剂：2-[[(4-Chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(un/located-phenyl)乙酰胺。,Pakistan journal of pharmaceutical sciences

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报告 - 合成有前景的抗菌剂和抗真菌剂：2-[[(4-Chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(un/located-phenyl)乙酰胺。
Pakistan journal of pharmaceutical sciences Pub Date : 2020-09-01
Muhammad Athar Abbasi ₁ , Misbah Irshad ₂ , - Aziz-Ur-Rehman ₁ , Sabahat Zahra Siddiqui ₁ , Majid Nazir ₁ , Syed Adnan Ali Shah ₃ , Muhammad Shahid ₄

Affiliation

在所提出的工作中，2,3-二氢-1,4-苯二恶英-6-胺 (1) 与 4-氯苯磺酰氯 (2) 在碱性水性介质存在下反应得到 4-氯-N-(2 ,3-二氢-1,4-苯并二恶英-6-基)苯磺酰胺(3)。同时，将各种未/取代的苯胺 (4a-1) 在碱化水性介质中用溴乙酰溴 (5) 处理以获得相应的 2-溴-N-(未/取代) 苯基乙酰胺 (6a-1) 作为亲电子试剂。然后化合物3最终与这些亲电子试剂6a-l在二甲基甲酰胺（DMF）为溶剂，氢化锂为碱和活化剂中反应合成各种2-[[（4-氯苯基）磺酰基]（2,3-二氢-1,4-苯并二恶英-6-基)氨基]-N-(未/取代的)苯基乙酰胺(7a-1)。合成的化合物经 IR、1H-NMR 和 EI-MS 光谱数据证实，用于结构确认。然后评估这些分子的抗微生物和抗真菌活性以及它们的溶血活性百分比。发现一些化合物具有合适的抗菌和抗真菌潜力，尤其是化合物 2-[[(4-氯苯基)磺酰基](2,3-二氢-1,4-苯并二恶英-6-基)氨基]-N-(3 ,5-二甲基苯基)乙酰胺 (7l) 表现出良好的抗菌潜力，但溶血活性的百分比值较低。

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REPORT - Synthesis of promising antibacterial and antifungal agents: 2-[[(4-Chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(un/substituted-phenyl)acetamides.

In the presented work, 2,3-dihydro-1,4-benzodioxin-6-amine (1) was reacted with 4-chlorobenzenesulfonyl chloride (2) in presence of aqueous basic aqueous medium to obtain 4-chloro-N-(2,3-dihydro-1,4-benzodioxin-6-yl)benzenesulfonamide (3). In parallel, various un/substituted anilines (4a-l) were treated with bromoacetyl bromide (5) in basified aqueous medium to obtain corresponding 2-bromo-N-(un/substituted)phenylacetamides (6a-l) as electrophiles. Then the compound 3 was finally reacted with these electrophiles, 6a-l, in dimethylformamide (DMF) as solvent and lithium hydride as base and activator to synthesize a variety of 2-[[(4-chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(un/substituted)phenylacetamides (7a-l). The synthesized compounds were corroborated by IR, 1H-NMR and EI-MS spectral data for structural confirmations. These molecules were then evaluated for their antimicrobial and antifungal activities along with their %age hemolytic activity. Some compounds were found to have suitable antibacterial and antifungal potential, especially the compound 2-[[(4-chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(3,5-dimethylphenyl)acetamide (7l) exhibited good antimicrobial potential with low value of % hemolytic activity.

更新日期：2020-09-01

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