title: Synthesis and antimicrobial activity of some new N-substituted quinoline derivatives of 1H-pyrazole.
abstract: 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.
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, Gujarat, India.
authors.forename: Nilesh J
authors.initials: NJ
authors.lastname: Thumar
authors.forename: Manish P
authors.initials: MP
authors.lastname: Patel
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D008826:Microbial Sensitivity Tests / Q000379:methods*; D015394:Molecular Structure; D011720:Pyrazoles / Q000737:chemistry*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D011720:Pyrazoles; D011804:Quinolines; C031280:pyrazole