title: Synthesis, characterization, and antimicrobial evaluation of carbostyril derivatives of 1H-pyrazole.
abstract: A new series of 12 derivatives of 4-pyrazolyl-N-arylquinoline-2,5-dione (4a-l) were synthesized by one pot base catalyzed cyclocondensation reaction of 1-aryl-5-chloro-3-methyl-1H-pyrazole-4-carbaldehyde (1a-c), Meldrum's acid (2) and 3-arylamino-5,5-disubstitutedcyclohex-2-enone (3a-d). All the compounds were characterized by elemental analysis, FT-IR, (1)H NMR and (13)C NMR spectral data and 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 (minimum inhibitory concentration) method. Some of the compounds were found to be equipotent or more potent than commercial drugs, against most of the employed strains, as evident from the screening data.
authors: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, 388120 Gujarat, India.
authors: Nilesh J
authors: NJ
authors: Thumar
authors: Manish P
authors: MP
authors: Patel
keywords: 1H-Pyrazole-4-carbaldehyde; Antimicrobial activity; Carbostyril; Minimum inhibitory concentration; Multicomponent reaction
references: Bioorg Med Chem. 2007 Oct 15;15(20):6527-34
references: 17689252
references: J Nat Prod. 2005 Sep;68(9):1397-9
references: 16180822
references: J Nat Prod. 2001 Dec;64(12):1579-80
references: 11754619
references: Bioorg Med Chem Lett. 2008 Feb 15;18(4):1431-5
references: 18207396
references: J Med Chem. 2005 Jan 13;48(1):192-9
references: 15634013
references: Eur J Med Chem. 2008 Mar;43(3):456-63
references: 17532544
references: Bioorg Med Chem Lett. 2008 Jul 1;18(13):3787-9
references: 18524583
references: J Nat Prod. 2004 Nov;67(11):1800-3
references: 15568765
references: Eur J Med Chem. 2007 Jul;42(7):934-9
references: 17321008
references: Bioorg Med Chem Lett. 2000 Apr 17;10(8):839-41
references: 10782698
references: Eur J Med Chem. 2002 Aug;37(8):671-9
references: 12161064
references: Chem Pharm Bull (Tokyo). 2003 Jul;51(7):838-44
references: 12843591
references: Bioorg Med Chem. 2001 Aug;9(8):2129-37
references: 11504649
references: Bioorg Med Chem Lett. 2007 Mar 15;17(6):1523-6
references: 17257838
references: Clin Infect Dis. 2002 Nov 1;35(9):1073-80
references: 12384841
references: Bioorg Med Chem. 2007 Mar 1;15(5):1947-58
references: 17240153
references: Eur J Med Chem. 2008 Aug;43(8):1730-6
references: 18164518
references: Bioorg Med Chem. 2003 Mar 20;11(6):1031-4
references: 12614889
references: Arch Pharm (Weinheim). 2011 Feb;344(2):91-101
references: 21290425
references: Bioorg Med Chem Lett. 2006 Jun 1;16(11):2925-8
references: 16563758
references: Thromb Res. 1989 Nov 1;56(3):333-46
references: 2559492
references: J Med Chem. 2002 Jun 6;45(12):2543-55
references: 12036363
references: J Am Chem Soc. 1948 Oct;70(10):3426-8
references: 18891879
references: Bioorg Med Chem Lett. 2009 Feb 15;19(4):1093-6
references: 19167220