A reassessment of mycophenolic acid as a lead compound for the development of inhibitors of chikungunya virus replication

Authors

Adel Rashad, University of WollongongFollow
Johan Neyts, University of Leuven
Pieter Leyssen, University of Leuven
Paul A. Keller, University of WollongongFollow

RIS ID

123207

Publication Details

Rashad, A. A., Neyts, J., Leyssen, P. & Keller, P. A. (2018). A reassessment of mycophenolic acid as a lead compound for the development of inhibitors of chikungunya virus replication. Tetrahedron, 74 (12), 1294-1306.

Abstract

Mycophenolic acid (MPA) has been previously reported as an inhibitor of the chikugunya virus (CHIKV) with an EC₅₀ value of 0.2 μM. We used MPA as a lead compound designing and synthesizing a series of isatins and benzolactones in a typical medicinal chemistry program. The synthesis and testing of 19 derivatives produced compounds with no desired activity which prompted us to retest the lead compound, MPA. We can reveal that MPA shows no anti-CHIKV activity and therefore needs to be reassessed as a lead compound for this target.