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Microwave assisted synthesis and characterization of certain novel bipyrazole derivatives and their antimicrobial activities
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UPLOADED BY-ADMIN, DHANYA B, UJJWAL SAHOO, A.K.SETH, A.K.SEN, S.KUMAR, Y.C.YADAV, T.K.GHELANI, R.CHAWLA
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| Abstract:
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The increasing clinical importances of drug resistant bacterial and fungal pathogens have lent an additional
urgency in the field of microbiological research and development of new antimicrobial comTpounds.
Microwave assisted synthesis is less time consuming and environmental friendly as compared to
the existing conventional method of synthesis. Pyrazoles possesses various biological activities such as
antibacterial, antifungal, antiviral, antitubercular, antidepressant, anti amoebic, anti-inflammatory, anticonvulsant
, analgesic and anticancer activity. In light of these interesting biological activities, it was our
interest to synthesize some novel bipyrazole derivatives 4 (a-f). Hydrazone derivatives 1(a-f) have been
prepared by reacting INH (Isonicotinic acid hydrazide) with substituted acetophenone. 1(a-f) were treated
with POCl3/DMF to afford pyrazole aldehyde derivatives 2(a-f). 2(a-f) were further treated with substituted
acetophenone in the presence of C2H5OH/NaOH gave substituted chalcones 3(a-f) and in the presence
of INH (Isonicotinic acid hydrazide) gave substituted bipyrazole derivatives 4(a-f). The structure of
newly synthesized compounds 4(a-f) have been confirmed by IR, and 1H NMR. All compounds have
been screened in vitro for their antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherchia
coli and Pseudomonas aeruginosa, and also for their antifungal activity against Candida albicans
and Asperigillus niger. Among the synthesized compounds, 4b, 4c and 4f showed better activity
against Candida albicans and compounds, 4a, 4e and 4f showed better activity than rest of compounds
against Asperigillus niger when compared with standard drug. Thus, microwave heating technology in
drug synthesis should be promoted in order to reducing the cost of basic drugs and chemicals.
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| Keyword:
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bipyrazoline, isonicotinic acid hydrazide, antifungal, antibacterial
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