1. Academic Validation
  2. Synthesis and antiviral activity of new pyrazole and thiazole derivatives

Synthesis and antiviral activity of new pyrazole and thiazole derivatives

  • Eur J Med Chem. 2009 Sep;44(9):3746-53. doi: 10.1016/j.ejmech.2009.03.038.
Osama I el-Sabbagh 1 Mohamed M Baraka Samy M Ibrahim Christophe Pannecouque Graciela Andrei Robert Snoeck Jan Balzarini Adel A Rashad
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. elsabbagh_59@yahoo.com
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.

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