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Synthesis and Antimicrobial Activity of Some New N ‐Substituted Quinoline Derivatives of 1 H ‐Pyrazole
Author(s) -
Thumar Nilesh J.,
Patel Manish P.
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000010
Subject(s) - antimicrobial , broth microdilution , chemistry , candida albicans , bacillus subtilis , malononitrile , vibrio cholerae , clostridium tetani , aspergillus fumigatus , pyrazole , aryl , escherichia coli , microbiology and biotechnology , stereochemistry , organic chemistry , bacteria , minimum inhibitory concentration , biology , catalysis , biochemistry , genetics , vaccination , alkyl , tetanus , gene , immunology
A new series of 32 derivatives of 4‐pyrazolyl‐ N ‐(hetero)arylquinoline 5a–p and 6a–p were synthesized by a one‐pot base‐catalyzed cyclocondensation reaction of 1‐phenyl‐3‐(hetero)aryl‐pyrazole‐4‐carbaldehyde 1a–h , malononitrile 2 , and 3‐(hetero)aryl‐5,5‐disubstitutedcyclohex‐2‐enone 3a–b or 4a–b , respectively. All the synthesized compounds were characterized by elemental analysis, FT‐IR, 1 H‐NMR, and 13 C‐NMR spectral data. All the synthesized compounds were screened, against six bacterial pathogens, namely Bacillus subtilis , Clostridium tetani , Streptococcus pneumoniae , Salmonella typhi , Vibrio cholerae , Escherichia coli , and antifungal activity, against two fungal pathogens Aspergillus fumigatus and Candida albicans , using broth microdilution MIC method. Some of the compounds were found to be more or equipotent against most of the employed strains than commercially available drugs as evident from the screening data.