Title: Synthesis and antiviral activity of new pyrazole and thiazole derivatives
Authors: El-Sabbagh, Osama I ×
Baraka, Mohamed M
Ibrahim, Samy M
Pannecouque, Christophe
Andrei, Graciela
Snoeck, Robert
Balzarini, Jan
Rashad, Adel A #
Issue Date: Sep-2009
Series Title: European Journal of Medicinal Chemistry vol:44 issue:9 pages:3746-3753
Abstract: New N-acetyl (5-8) and N-thiocarbamoyl (9-12) derivatives of 4,5-dihydropyrazole were synthesized starting from alpha,beta-unsaturated ketones under the effect of hydrazine hydrate and thiosemicarbazide, respectively. N-Thiocarbamoylpyrazole derivatives (9-12) were cyclized using either ethyl bromoacetate or phenacyl bromides to afford the novel pyrazolothiazol-4(5H)-ones (13-16) or pyrazolothiazoles (17-24). The antiviral activity for such novel compounds against a broad panel of viruses in different cell cultures revealed that N-acetyl 4,5-dihydropyrazole 7 was the only active one at subtoxic concentrations against vaccinia virus (Lederle strain) in HEL cell cultures with a 50% effective concentration (EC(50)) value of 7 microg/ml.
ISSN: 0223-5234
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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