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Title: Antimicrobial and antinociceptive profile of some novel pyrazole derivatives
Authors: Sen, Sandip
Bhaumik, Pradip
Roy, Biswabara
Easwari, T S
Choudhury, Ratna
Mallik, Arunabha
De, Biplab
Keywords: Antimicrobial;Analgesic;Azetidine-2-one;Pyrazole-4-carboxaldehyde
Issue Date: Apr-2016
Publisher: NISCAIR-CSIR, India
Abstract: A new series of 4-(3-methyl-1H-pyrazol-4-yl)-1-phenylazetidin-2-ones 6a-j have been prepared by intermolecular cyclization of Schiff bases 5a-j and monochloro acetyl chloride in the presence of a base catalyst triethylamine. The 1H and 13C NMR data show the presence of E isomer of Schiff bases 5a-j. Structures of all the synthesized compounds have been confirmed by spectral analysis. The biological evaluation of the compounds like antimicrobial, analgesic have been performed. From the biological investigation, it is found that out of all the synthesized compounds 6a, 6b, 6d, 6f and 6j show potent antimicrobial and anti-nociceptive activity. The SAR study confirms the presence of azetidine-2-one nucleus along with pyrazole nucleus essential for the activity. However, in particular, efficacy depends on substitution at phenyl ring, attached to the azetidine-2-one nucleus.
Page(s): 507-516
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.55B(04) [April 2016]

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