5-Arylidene-2,4-thiazolidinedione (5-A-TZD) is an emerging precursor molecule in medicinal chemistry for discovering multifunctional therapeutic agents. For synthesizing this precursor molecule, Knoevenagel Condensation (KC) is one of the most excellent tools in modern organic chemistry. The 5-A-TZD framework has a variety of therapeutic functions such as antidiabetic, anticancer, antimicrobial, and anti-inflammatory. As a result, several approaches and methods of KC have been established for the synthesis of this multifunctional precursor. However, the use of highly corrosive catalysts, prolonged reaction times, by-products formation, and poor product yields are the main drawbacks in 5-A-TZDs synthesis via KC. Therefore, several authors have been successfully established fast, effective, and environmentally sustainable protocols of KC using organic catalysts, inorganic catalysts, heterogeneous solid catalysts, ionic liquids (ILs), and bio-catalysts to synthesize 5-A-TZD derivatives with high conversion yield and selectivity. In this review, we have summarized the recent approaches for synthesizing 5-A-TZDs via KC and their therapeutic application as a precursor molecule in medicinal chemistry.
25 November 2023 in European Journal of Medicinal Chemistry
Indazole is a vital nitrogen-containing heterocyclic unit in organic and medicinal chemistry research and a helpful precursor molecule for the production of various types of encirclement heterocycles. Indazole analogues are diverse pharmacological agents that can be used to treat a variety of conditions, including cancer, inflammation, infectious diseases, and neurological problems. In fact, the indazole moiety containing inhibitors also showed excellent medicinal properties for the treatment of parasitic diseases. Therefore, the development of new inhibitors has immense promise for usage as key components for the next generation as antiparasitic medication. In this review, we have summarized the recent developments of indazole-containing antiparasitic inhibitors, specially anti-protozoal, anti-fungal, and antiamoebic inhibitors, as well as their structure-activity relationship (SAR) findings for medicinal chemists who are searching for new preclinical parasitic drug candidates.