The design, synthesis, and in vitro trypanocidal and leishmanicidal activities of 1,3-thiazole and 4-thiazolidinone ester derivatives

Abstract

Chagas and leishmaniasis are both neglected tropical diseases, whose inefficient therapies have made them remain the cause for millions of deaths worldwide.

Synthesis and in Silico Docking Studies of Ethyl 2‐(2‐Arylidene‐1‐alkylhydrazinyl)thiazole‐4‐carboxylates as Antiglycating Agents

“…A multistep sequence was followed to obtain ethyl 2‐(arylidene‐1‐alkylhydrazinyl)thiazole‐4‐carboxylates ( 1a – k ). The compounds ( 1a– k) were synthesized by simple substitution reaction on ethyl 2‐(2‐arylidenehydrazinyl)thiazole‐4‐carboxylates [34] by alkyl halides in the presence of potassium carbonate under reflux as presented in Scheme 1. The initial verification of all synthesized compounds ( 1a – k ) was carried out with different physical parameters.…”

“…Another, one proton singlet corresponding to azomethine (−CH=N−) moiety was observed at 7.96–8.21 ppm. The assignment of thiazole ring and azomethine proton is based on the literature values [34] . All aromatic proton signals were found at their respective positions with respect to substituents attached to the benzene ring and did not exhibit any significant change after alkylation.…”

Synthesis of Arylidenehydrazinyl‐4‐methoxyphenylthiazole Derivatives: Docking Studies, Probing Type II Diabetes Complication Management Agents

“…The up‐field carbon signals in range δ 55.3–56.2 ppm were assigned to the methoxy carbons. The synthesis of compounds was further confirmed when NMR spectra were compared with literature reported similar skeleton compounds [38–45] …”

“…The synthesis of compounds was further confirmed when NMR spectra were compared with literature reported similar skeleton compounds. [38][39][40][41][42][43][44][45] After establishing the synthesis of the expected hydrazinyl-4-methoxyphenylthiazoles their biological significance was investigated by α-amylase inhibitory potential, antiglycation activity, antioxidant potential and cytotoxic behaviour by haemolytic assay.…”

The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies

“…These values were better than those for standard benzimidazole (EC50 = 34.5 µM). Furthermore, the Compounds 97a and 97b demonstrated better IC50 values for both Leishmania amazonensis (IC50 = 14.63 and 13.35 µM) and Leishmania infantum (IC50 = 14.63 and 13.35 µM) in comparison with reference drug miltefosine (36.31 and 53.71 µM) [107].…”