Synthesis and screening of some novel fused thiophene and thienopyrimidine derivatives for anti-avian influenza virus (H5N1) activity

• DOI: 10.1016/j.ejmech.2010.08.044
• Publication Date: 2010-08-25T08:38:12Z
• Authors: Aymn E. Rashad; Ahmed H. Shamroukh; Randa E. Abdel-Me...; Ahmed Mostafa; Rabeh El-Shesheny; Ahmed Kandeil; Mohamed A. Ali; Klaus Banert
• Keywords: Structure-Activity Relationship; Magnetic Resonance Spectroscopy; Pyrimidines; Influenza A Virus, H5N1 Subtype; Spectrophotometry, Infrared; Thiophenes; Antiviral Agents; 01 natural sciences; Mass Spectrometry; 0104 chemical sciences; 3. Good health

Several derivatives containing dihydronaphtho, naphtho[2,1-b]thiophene and thieno[2,3-d]pyrimidine ring systems were prepared starting from 2-amino-4,5-dihydronaphtho[2,1-b]thiophene-1-carbonitrile (1). Structure characterization of the thioxo derivative 7 was also performed and its reaction with some chloro and bromoalkyl reagents was studied. Moreover, the prepared products were tested for antiviral activity against H5N1 virus [A/chicken/Egypt/1/2006 (H5N1)] by determination of both EC50 and LD50 and confirmed by plaque reduction assay on MDCK cells. Compounds 5, 7 and 8 showed the highest effect compared with the other tested compounds.