Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening

European Journal of Medicinal Chemistry
2014.0

Abstract

A novel series of fluoro substituted pyrazolylpyrazolines 7a-l was synthesized in good to excellent yield (77-88%) from pyrazole chalcones 5a-d and substituted phenyl hydrazine hydrochlorides 6a-c under microwave irradiation. The newly synthesized compounds were screened for their preliminary in vitro antibacterial activity against a panel of pathogenic stains of bacteria and fungi, antituberculosis activity against Mycobacterium tuberculosis H37Rv and antimalarial activity against Plasmodium falciparum. Compounds 7a, 7b, 7g, 7h, 7j and 7k displayed excellent activity against P. falciparum stain as compared to quinine IC50 0.268. Good antitubercular activity was exhibited by compounds 7a, 7e, 7h and 7k. Some of them also exhibited superior antibacterial activity as compared to the first line drugs.

Knowledge Graph

Similar Paper

Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening
European Journal of Medicinal Chemistry 2014.0
Novel morpholinoquinoline nucleus clubbed with pyrazoline scaffolds: Synthesis, antibacterial, antitubercular and antimalarial activities
European Journal of Medicinal Chemistry 2016.0
Green synthesis and anti-infective activities of fluorinated pyrazoline derivatives
Bioorganic & Medicinal Chemistry Letters 2012.0
Synthesis, antitubercular and antimicrobial evaluation of 3-(4-chlorophenyl)-4-substituted pyrazole derivatives
Bioorganic & Medicinal Chemistry Letters 2012.0
Synthesis of 1,3,5-trisubstituted pyrazolines as potential antimalarial and antimicrobial agents
Bioorganic & Medicinal Chemistry 2017.0
Thermal solvent-free synthesis of novel pyrazolyl chalcones and pyrazolines as potential antimicrobial agents
Bioorganic & Medicinal Chemistry Letters 2011.0
Synthesis, identification and in vitro biological evaluation of some novel quinoline incorporated 1,3-thiazinan-4-one derivatives
Bioorganic & Medicinal Chemistry Letters 2017.0
Synthesis of novel quinoline–based 4,5–dihydro–1 H –pyrazoles as potential anticancer, antifungal, antibacterial and antiprotozoal agents
European Journal of Medicinal Chemistry 2017.0
Substituted quinolinyl chalcones and quinolinyl pyrimidines as a new class of anti-infective agents
European Journal of Medicinal Chemistry 2009.0
Synthesis, characterization and pharmacological screening of some novel 5-imidazopyrazole incorporated polyhydroquinoline derivatives
European Journal of Medicinal Chemistry 2014.0