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

Journal Article


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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.

Authors


  •   Rashad, Adel (external author)
  •   Neyts, Johan (external author)
  •   Leyssen, Pieter (external author)
  •   Keller, Paul A.

Publication Date


  • 2018

Citation


  • 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.

Scopus Eid


  • 2-s2.0-85042711402

Ro Full-text Url


  • http://ro.uow.edu.au/cgi/viewcontent.cgi?article=6351&context=smhpapers

Ro Metadata Url


  • http://ro.uow.edu.au/smhpapers/5297

Number Of Pages


  • 12

Start Page


  • 1294

End Page


  • 1306

Volume


  • 74

Issue


  • 12

Place Of Publication


  • United Kingdom

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.

Authors


  •   Rashad, Adel (external author)
  •   Neyts, Johan (external author)
  •   Leyssen, Pieter (external author)
  •   Keller, Paul A.

Publication Date


  • 2018

Citation


  • 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.

Scopus Eid


  • 2-s2.0-85042711402

Ro Full-text Url


  • http://ro.uow.edu.au/cgi/viewcontent.cgi?article=6351&context=smhpapers

Ro Metadata Url


  • http://ro.uow.edu.au/smhpapers/5297

Number Of Pages


  • 12

Start Page


  • 1294

End Page


  • 1306

Volume


  • 74

Issue


  • 12

Place Of Publication


  • United Kingdom