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   Synthesis of biologically active O-substituted derivatives of 1-[(3, 5-dichloro-2-hydroxyphenyl)sulfonyl]piperidine  
   
نویسنده Khalid Hira ,ur-Rehman Aziz ,Abbasi Muhammad Athar ,Khan Khalid Mohammad ,Ashraf Muhammad ,Ahmad Irshad ,Ejaz Abida
منبع pakistan journal of pharmaceutical sciences - 2013 - دوره : 26 - شماره : 3 - صفحه:479 -485
چکیده    In the present work, a series of 2-o-substituted derivatives of 1-[(3,5-dichloro-2-hydroxy phenyl) sulfonyl]piperidine (5a-j) were synthesized. these derivatives were geared up by the coupling of 3,5-dichloro-2-hydroxy benzenesulfonyl chloride (1) with piperidine (2) under dynamic ph control in aqueous media to form parent compound 1-[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]piperidine (3), followed by the substitution at oxygen atom with different electrophiles (4a-j) in the presence of sodium hydride (nah) and dimethyl formamide (dmf) to give a series of osubstituted derivatives of sulfonamides bearing piperidine nucleus 5a-j. the synthesized o-substituted sulfonamides were spectrally characterized. the bioactivity of all the synthesized compounds were evaluated against lipoxygenase (lox), acetylcholinesterae (ache) and butyrylcholinesterase (bche) enzymes and found to be having talented activity against butyrylcholinesterase enzyme.
کلیدواژه Piperidine ,5-dichloro-2-hydroxybenzenesulfonyl chloride ,enzyme inhibition activity ,1H-NMR ,EI-MS
آدرس Government College University, Department of Chemistry, Pakistan, Government College University, Department of Chemistry, Pakistan, Government College University, Department of Chemistry, Pakistan, University of Karachi, HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, Pakistan, Islamia University of Bahawalpur, Department of Biochemistry and Biotechnology, Pakistan, Islamia University of Bahawalpur, Department of Pharmacy, Pakistan, Islamia University of Bahawalpur, Department of Pharmacy, Pakistan
 
     
   
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