Synthesis and in-vitro evaluation of 2-amino-4-arylthiazole as inhibitor of 3D polymerase against foot-and-mouth disease (FMD)

• One of the targets to suppress expansion of and to control FMD is 3D polymerase.
• HTS campaign with in-house chemical library presented Hit compounds.
• 2-Amino-4-arylthiazoles were synthesized for the inhibitor of 3D polymerase.
• The derivatives showed potent anti-viral activity against FMDV.

Foot-and-mouth disease (FMD) is a highly contagious vesicular disease of livestock caused by a highly variable RNA virus, foot-and-mouth disease virus (FMDV). One of the targets to suppress expansion of and to control FMD is 3D polymerase (FMDV 3Dpol). In this study, 2-amino-4-arylthiazole derivatives were synthesized and evaluated for their inhibitory activity against FMDV 3Dpol. Among them, compound 20i exhibited the most potent functional inhibition (IC50 = 0.39 μM) of FMDV 3D polymerase and compound 24a (EC50 = 13.09 μM) showed more potent antiviral activity than ribavirin (EC50 = 1367 μM) and T1105 (EC50 = 347 μM) with IBRS-2 cells infected by the FMDV O/SKR/2010 strain.

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