Synthesis and pharmacological evaluation of some novel 2-(5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles

European Journal of Medicinal Chemistry
2013.0

Abstract

A series of novel 2-(5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles (6) were synthesized by condensing 3-(2-bromoacetyl)coumarins (4) with various 5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-thiocarboxamides (5), obtained by the reaction of thiosemicarbazide with trifluoromethyl-β-diketones. All the tested compounds displayed significant to moderate in vivo anti-inflammatory activity when compared to the standard drug indomethacin, and good broad spectrum in vitro antibacterial activity against three Gram-positive and four Gram-negative bacteria when compared with cefixime.

Knowledge Graph

Similar Paper

Synthesis and pharmacological evaluation of some novel 2-(5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles
European Journal of Medicinal Chemistry 2013.0
Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents
Bioorganic & Medicinal Chemistry Letters 2012.0
Synthesis and biological evaluation of some pyrazole derivatives as anti-inflammatory–antibacterial agents
Medicinal Chemistry Research 2012.0
Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory–antimicrobial agents
Bioorganic & Medicinal Chemistry Letters 2015.0
Synthesis, biological evaluation and molecular modeling study of 5-trifluoromethyl-Δ2-pyrazoline and isomeric 5/3-trifluoromethylpyrazole derivatives as anti-inflammatory agents
European Journal of Medicinal Chemistry 2013.0
Synthesis and pharmacological evaluation of a novel series of 5-(substituted)aryl-3-(3-coumarinyl)-1-phenyl-2-pyrazolines as novel anti-inflammatory and analgesic agents
European Journal of Medicinal Chemistry 2009.0
Synthesis and biological evaluation of some novel thiazole compounds as potential anti-inflammatory agents
European Journal of Medicinal Chemistry 2013.0
Design and microwave-assisted synthesis of 5-trifluoromethyl-4,5-dihydro-1H-pyrazoles: Novel agents with analgesic and anti-inflammatory properties
European Journal of Medicinal Chemistry 2008.0
Design and synthesis of 3-pyrazolyl-thiophene, thieno[2,3-d]pyrimidines as new bioactive and pharmacological activities
Bioorganic & Medicinal Chemistry Letters 2008.0
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents
European Journal of Medicinal Chemistry 2008.0