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Here, we report the chemical synthesis of two DPDPE analogues  7a  ( NOVA1)  and  7b  ( NOVA2 ). This entailed the solid-phase synthesis of two enkephalin precursor chains followed by a Cu I -catalyzed azide-alkyne cycloaddition, with the aim of improving  in vivo  analgesic efficacy versus DPDPE.  NOVA2  showed good affinity and selectivity for the μ-opioid receptor (K I  of 59.2 nM, EC 50  of 12.9 nM, E Max  of 87.3%), and long lasting anti-nociceptive effects in mice when compared to DPDPE.

On resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity