Facile synthesis of novel fluorine containing pyrazole based thiazole derivatives and evaluation of antimicrobial activity

• Published in: Journal of fluorine chemistry Vol. 142; pp. 67 - 78
• Main Authors: Desai, N.C., Joshi, V.V., Rajpara, K.M., Vaghani, H.V., Satodiya, H.M.
• Format: Journal Article
• Language: English
• Published: LAUSANNE Elsevier B.V 01.10.2012; Elsevier
• Subjects: Antibacterial activity; Antifungal activity; Antiinfectives and antibacterials; Aspergillus niger; Bacteria; Candida albicans; Chemistry; Chemistry, Inorganic & Nuclear; Chemistry, Organic; Derivatives; Escherichia coli; Fluorine; Mass spectra; MIC; Nuclear magnetic resonance; Panels; Physical Sciences; Pseudomonas aeruginosa; Pyrazole; Pyrazoline; Science & Technology; Staphylococcus aureus; Streptococcus pyogenes; Thiazole; Antifungal activity; Antibacterial activity; Pyrazoline; Thiazole; MIC; Pyrazole; ANTIDEPRESSANT; ANALOGS; IDENTIFICATION; 3,5-DIARYL PYRAZOLINES; MEDICINAL CHEMISTRY; POTENT; INHIBITORS
• ISSN: 0022-1139; 1873-3328
• DOI: 10.1016/j.jfluchem.2012.06.021

A novel series of 2-(5-(3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)-3-(aryl)-4,5-dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-ones (4a–q) were prepared and screened for in vitro antimicrobial activity. [Display omitted] ► Describe facile synthesis of fluorine containing pyrazole based thiazole compounds. ► Compounds were screened for their in vitro antimicrobial activity. ► Compounds were characterized adequately by various spectral data and CHN analysis. ► Newly synthesized compounds exhibited potential antimicrobial activity. A series of compounds 2-(5-(3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)-3-(aryl)-4,5-dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-ones (4a–q) were synthesized and structures of these compounds were elucidated by spectral (IR, 1H NMR, 13C NMR, mass spectra) analysis. Synthesized compounds were screened for in vitro antibacterial activity against the representative panel of Gram-positive (Staphylococcus aureus, Streptococcus pyogenes) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria. These compounds were also tested for their inhibitory action against strains of fungi (Candida albicans, Aspergillus niger, Aspergillus clavatus). The synthesized compounds showed potent inhibitory action against the test organisms.