Design, Synthesis and Preliminary Evaluation of Novel Imperatorin Derivatives as Vasorelaxant Agents

Article abstract of DOI:10.2174/157340611794072715

A series of novel imperatorin derivatives were synthesized from commercially available xanthotoxin. The in vitro pharmacological evaluation indicated that all of the compounds possessed potent vasodilatory activity. Among them, compounds (5b), (5d) and (5e) exhibited higher vasdilatory activity (with EC₅₀ values of 0.68 μM, 0.59 μM and 0.49 μM, respectively) than imperatorin (EC₅₀ = 1.12 μM). The program Volsurf was used to predict the derivatives' ADMErelevant descriptors. The results suggested that these novel compounds had a potential interest for the development of novel and potent vasorelaxant agents.