HIV-1 replication inhibitors of the styrylquinoline class: introduction of an additional carboxyl group at the C-5 position of the quinoline

Abstract

Novel variants of HIV-1 replication inhibitors of the styrylquinoline class, bearing an additional acid group or a propenoic acid moiety at the C-5 position of the quinoline have been synthesized. Key steps included Heck reaction and palladium catalyzed carbonylation reaction of 5-haloquinaldine derivatives. These compounds exhibited reinforced anti-integrase potency and significant antiviral activities.