title: Synthesis and biological evaluation of some 4-functionalized-pyrazoles as antimicrobial agents.
abstract: 1,3-Diaryl-4-formylpyrazoles 8 bearing benzenesulfonamide moiety at position-1 were synthesized as important intermediates following Vilsmeier-Haack strategy. Aldehyde moiety of 4-formylpyrazole was then converted into carboxylic acid 9, cyano 10 and carbothioamide 11 using established procedures. Out of these 4-functionalized pyrazoles, pyrazole-4-carboxylic acids 9 and carbothioamides 11 were evaluated for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacillus subtilis (Gram-positive), Escherichia coli, Pseudomonas aeruginosa (Gram-negative), and in vitro antifungal activity against two pathogenic fungal strains namely, Aspergillus niger and Aspergillus flavus. Three tested compounds, 9e, 11b and 11f exhibited moderate antibacterial activity against Gram-positive bacteria and 9g showed moderate antifungal activity against the tested fungi. However, none of the compounds showed any activity against Gram-negative bacteria.
authors.affiliation: Department of Chemistry, Kurukshetra University, Kurukshetra 136 119, India. talk2pawan@gmail.com
authors.forename: Pawan K
authors.initials: PK
authors.lastname: Sharma
authors.forename: Navneet
authors.initials: N
authors.lastname: Chandak
authors.forename: Pawan
authors.initials: P
authors.lastname: Kumar
authors.forename: Chetan
authors.initials: C
authors.lastname: Sharma
authors.forename: Kamal R
authors.initials: KR
authors.lastname: Aneja
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D002264:Carboxylic Acids / Q000737:chemistry; D005658:Fungi / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013449:Sulfonamides / Q000737:chemistry; D000096926:Benzenesulfonamides
chemical_list: D000890:Anti-Infective Agents; D002264:Carboxylic Acids; D011720:Pyrazoles; D013449:Sulfonamides; D000096926:Benzenesulfonamides