Synthesis of N-benzyl-N-phenylthiophene-2-carboxamide analogues as a novel class of enterovirus 71 inhibitors

摘要: A series of novel human enterovirus 71 inhibitors, N-benzyl-N-phenylthiophene-2-carboxamide analogues, were synthesized and their antiviral activities evaluated in vitro. Most derivatives this structure against EV71 had a low micromolar range the RD (rhabdomyosarcoma) cell lines. The most potent compound 5a, N-(4-bromobenzyl)-N-(4-fluorophenyl)thiophene-2-carboxamide, showed activity (EC50 = 1.42 μM) compared to reference anti-EV71 drug enviroxime 0.15 μM). Preliminary SAR studies revealed that thiophene-2-carboxamide core is crucial for maintaining activity, N-substituent phenyl groups largely influenced efficacy new class agents.