Novel 4-thiazolidinone derivatives bearing imidazo[2,1- b]thiazole moiety: design, synthesis, and antiviral activity evaluation

Abstract

This paper aimed to synthesize novel compounds carrying imidazo[2,1-b]thiazole nucleus, characterize them with various spectroscopic methods, moreover evaluate their antiviral activity. All novel derivatives were evaluated for their antiviral activity against Coxsackie B4 virus, Respiratory syncytial virus, Influenza A/H1N1 virus, Influenza A/H3N2, and Influenza B virus. Some of the compounds, particularly the derivatives carrying 4methylphenyl and 4-bromophenyl moiety, exhibited higher and comparable activities against both Coxsackie B4 and Respiratory syncytial viruses, moreover the compounds with N-propyl and N-butyl at thiazolidinone ring showed high antiviral activities against Influenza Influenza A/H3N2 viruses. Consequently, the results obtained from in vitro assay data shed light on improving novel antiviral.

A newly synthesized thiosemicarbazide derivative trigger apoptosis rather than necroptosis on HEPG2 cell line

“…(Basoglu & Ulusoy Guzeldemirci, 2020;Mohamed & Abdel-wahab, 2012;Shareef et al, 2020). Along with our work (Basoglu et al, 2021;Başoğlu-ünal et al, 2023;Dincel et al, 2020;Gursoy et al, 2020;Ulusoy Guzeldemirci et al, 2019;Ulusoy Guzeldemirci et al, 2017) regarding both scaffolds, many approved drug molecules by FDA are on the market such as Triapine, thioacetazone, methisazone (Dincel et al, 2021), and levamisole (Basoglu et al, 2021) which carry either thiosemicarbazide or imidazo[2,1-b]thiazole moiety. Levamisole was approved for the first time as an anticancer drug with an imidazo[2,1-b]thiazole structure (Basoglu et al, 2021).…”

“…This difference offers to distinguish thiosemicarbazide derivatives from hydrazide. All synthesized compounds showed wide and weak bands arising from N-H around 3251-3122 cm −1 region, whereas disappearing any two sharp bands resulting from NH 2 (Başoğlu-ünal et al, 2023;Erdik, 2015). Furthermore, there is one more difference of the designed molecules have arising from thiosemicarbazide scaffold which is C=S band as well.…”