A facile one-pot multi-component synthesis of novel adamantine substituted imidazo[1,2-a] pyridine derivatives: identification and structure-activity relationship study of their anti-HIV-1 activity

摘要

In this study, a series of adamantine substituted imidazo[1,2-a] pyridine derivatives were designed and synthesized through a one-pot multi-component Groebke-Blackburn-Bienayme reaction. Their anti-HIV activities were evaluated using an HIV-1(IIIB)/TZM-bl indicator cell culture system, in which compounds 19d, 19e and 19m were found to be the most potent inhibitors with EC50 values of 0.048, 0.061 and 0.077 mM, respectively. Furthermore, the modeling results provided valuable insight into how compound 19d gave good efficacy against HIV-1 cells.