Siddiqui Sabahat Zahra, Zahid Anam, Abbasi Muhammad Athar, Rehman Azizur, Nasim Faizul Hassan
Department of Chemistry, Government College University, Lahore, Pakistan.
Department of Chemistry, The Islamia University of Bhawalpur, Bhawalpur, Pakistan.
Pak J Pharm Sci. 2017 May;30(3):675-681.
A facile method has been implemented for the synthesis of different N-substituted sulfamoylacetamides by reacting 4-acetamidobenzenesulfonyl chloride (1) with different alkyl/aralkyl/aryl amines (2a-q) in basic aqueous media under controlled pH to afford -[(Substitutedsulfamoyl) phenyl]acetamides (3a-q) which were confirmed through spectral analysis like FT-IR, EIMS and H-NMR. Moreover, the synthesized derivatives were screened against α-Chymotrypsin. The enzyme inhibitory results revealed that most of the synthesized compounds were found to be moderate enzyme inhibitors.
通过在受控pH的碱性水性介质中使4-乙酰氨基苯磺酰氯（1）与不同的烷基/芳烷基/芳基胺（2a-q）反应，实现了一种简便的方法来合成不同的N-取代氨磺酰基乙酰胺，以得到-[(取代氨磺酰基)苯基]乙酰胺（3a-q），这些产物通过FT-IR、EIMS和H-NMR等光谱分析得到证实。此外，对合成的衍生物进行了α-胰凝乳蛋白酶筛选。酶抑制结果表明，大多数合成化合物是中等强度的酶抑制剂。
