Design, synthesis and evaluation of novel diaryl pyrrolopyrimidine and pyrrolothiazine derivatives as inhibitors of tumor necrosis factor stimulated gene-14 (TSG-14) production

• Synthesis of novel diaryl pyrrolopyrimidine and pyrrolothiazine derivatives.
• All compounds were characterized based on microanalytical and spectral data.
• The newly synthesized compounds were evaluated as inhibitors of TSG-14.
• Compounds 4e and 6e showed excellent potency in vivo (70% and 80% respectively).

A novel series of pyrrolothiazines 2–4 and pyrrolopyrimidines 5–7 have been synthesized. The structures of these compounds were established by spectroscopic and element microanalytical data. The newly synthesized compounds were evaluated as inhibitors of TSG-14. The most effective results were obtained by the S-sec-butyl derivatives 6e (80%) and the N-ethyl derivatives 4e (70%).

Synthesis of pyrrolothiazines and pyrrolopyrimidines.Figure optionsDownload as PowerPoint slide