2-Phenitidine derivatives as suitable inhibitors of butyrylcholinesterase

Authors

  • Muhammad Athar Abbasi Government College University; Department of Chemistry
  • Muhammad Athar Aziz-ur-Rehman Government College University; Department of Chemistry
  • Muhammad Zahid Qureshi Government College University; Department of Chemistry
  • Farhan Mehmood Khan Government College University; Department of Chemistry
  • Khalid Mohmmed Khan University of Karachi; International Center for Chemical and Biological Sciences; Research Institute of Chemistry
  • Muhammad Ashraf Department of Biochemistry and Biotechnology
  • Iftikhar Afzal The Islamia University of Bahawalpur; Department of Pharmacy

DOI:

https://doi.org/10.1590/S1984-82502013000100014

Keywords:

2-Phenitidine^i1^sinhibitor activ, Sulfonamides, Acetamide, Benzamide, Butyrylcholinesterase

Abstract

This manuscript reports the synthesis of a series of N-substituted derivatives of 2-phenitidine. First, the reaction of 2-phenitidine (1) with benzene sulfonyl chloride (2) yielded N-(2-ethoxyphenyl) benzenesulfonamide (3), which further on treatment with sodium hydride and alkyl halides (4a-g) furnished into new sulfonamides (5a-g). Second, the phenitidine reacted with benzoyl chloride (6) and acetyl chloride (8) to yield the reported N-benzoyl phenitidine (7) and N-acetyl phenitidine (9), respectively. These derivatives were characterized by infrared spectroscopy, ¹H-NMR, and EI-MS, and then screened against acetylcholinesterase, butylcholinesterase, and lipoxygenase enzyme, and were found to be potent inhibitors of butyrylcholinesterase alone.

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Published

2013-03-01

Issue

Section

Articles

How to Cite

2-Phenitidine derivatives as suitable inhibitors of butyrylcholinesterase . (2013). Brazilian Journal of Pharmaceutical Sciences, 49(1), 127-133. https://doi.org/10.1590/S1984-82502013000100014