Open AccessSynthesis, characterization and In vitro antimicrobial evaluation of novel pyrazolothiazol-4(5H)-one derivatives
Author(s) -
Priyanka L. Gaikwad,
Priyanka S Gandhi,
Deepali M. Jagdale,
Vilasrao J. Kadam
Publication year - 2013
Publication title -
indian journal of pharmaceutical sciences/indian journal of pharmaceutical sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.245
H-Index - 57
eISSN - 1998-3743
pISSN - 0250-474X
DOI - 10.4103/0250-474x.119830
Subject(s) - antimicrobial , chemistry , in vitro , bacteria , minimum inhibitory concentration , proton nmr , combinatorial chemistry , gram , organic chemistry , biochemistry , biology , genetics
Antimicrobial screening of several novel pyrazolothiazol-4(5H)-one derivatives (3a-3j) has been performed. Reaction of aromatic aldehydes with aromatic ketones yielded starting chalcones (1a-1j) which have been subsequently reacted with thiosemicarbazide for obtaining N-thiocarbamoylpyrazole derivatives (2a-2j). These were further cyclized to pyrazolothiazol-4(5H)-one derivatives (3a-3j) in the presence of ethylbromoacetate. The structures of newly synthesized compounds were confirmed by FTIR and (1)H NMR and/or MS. The in vitro antimicrobial activity of these compounds was evaluated against Gram positive bacteria, Gram negative bacteria and fungi. Their minimum inhibitory concentration was determined by tube dilution method. The results showed that most of the compounds have promising antimicrobial activity as compared to standard drugs. Among the test compounds, 2-[5(4-chlorophenyl)-3-phenyl-4,5-dihydropyrazol-1-yl]-thiazol-4(5H)-one (3e) was found to show the most potent antimicrobial activity.