Synthesis and Antiviral Activity of Chiral Thiourea Derivatives

Abstract

In conclusion, an eco-friendly green chemistry procedure in ionic liquid has been developed for the synthesis of novel chiral thiourea derivatives in high yields. The ionic solvent can be recovered and reused without any loss of its activity. This method is easy, rapid and good-yielding for the synthesis of title chiral compounds 3.3. The structures of the title compounds were verified by spectroscopic data. The preliminary bioassay showed that some of the chiral thiourea analogues exhibited moderate to good in vivo antiviral activities against TMV at 500 µg/mL. Title chiral compound 3.3i was found to possess good in vivo protection, inactivation and curative effects against TMV with inhibitory effects of 57.0%, 96.4%, 55.0% at 500 µg/mL. It was found that the title chiral compound 3.3i had better inactivation effect against TMV(EC50=50.8 ug/mL) than Ningnanmycin (EC50=60.2 µg/mL). To the best of our knowledge, this is the first report on the syntheses of chiral thiourea derivatives with antiviral activity in ionic solvent. Further studies are in progress to promote structural optimization and antiviral activities of the chiral thiourea analogues.