Synthesis of biologically active O-substituted derivatives of 1-[[3, 5-dichloro-2-hydroxyphenyl]sulfonyl]piperidine
Pakistan Journal of Pharmaceutical Sciences. 2013; 26 (3): 479-485
in English
| IMEMR
| ID: emr-142607
ABSTRACT
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
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Index:
IMEMR (Eastern Mediterranean)
Main subject:
Oxygen
/
Structure-Activity Relationship
/
Butyrylcholinesterase
/
Cholinesterase Inhibitors
/
Lipoxygenase Inhibitors
/
Lipoxygenase
/
Sodium Compounds
/
Hydrogen-Ion Concentration
Language:
English
Journal:
Pak. J. Pharm. Sci.
Year:
2013
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