Open AccessSynthesis, Characterization and Biological Activities of Pyrazole Based Heterocycles
Author(s) -
Nitin V. Kale,
S P Salve,
Bhaskar H. Zaware,
B. K. Karale,
Anil Athare,
Sushama B. Dare,
S. J. Takate
Publication year - 2022
Publication title -
asian journal of chemistry/asian journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.145
H-Index - 34
eISSN - 0975-427X
pISSN - 0970-7077
DOI - 10.14233/ajchem.2022.23556
Subject(s) - chemistry , thiophene , pyrazole , antifungal , antibacterial activity , biological activity , combinatorial chemistry , minimum inhibitory concentration , stereochemistry , organic chemistry , medicinal chemistry , antimicrobial , bacteria , in vitro , biochemistry , medicine , dermatology , biology , genetics
In this work, a unique pyrazolyl compounds comprising flourine and thiophene were synthesized. In brief, esters 3a-f were synthesizedby reacting thiophene and pyrazolyl acid (1) with various 2-hydroxyacetophenones (2a-f). The 1,3-diketones 4a-f were formed by Baker-Venkataraman rearrangement of esters 3a-f. Compounds 4a-f were cyclized to form chromene derivatives 5a-f, which further convertedinto pyrazolyl derivatives 6a-f. The majority of the compounds in series 3a-f, 4a-f, 5a-f and 6a-f showed promising antibacterial activityagainst S. typhii, S. aureus, B. subtilis and E. coli. Compounds 4e and 4f exhibited considerable antifungal activity against A. niger, whilethe majority of the compounds had promising activity against T. viride. At 1 mg/mL concentration, some of the synthesized compoundsshown potential α-amylase inhibitory action.