3‐Bromoacetylcoumarin, a Crucial Key for Facial Synthesis of Biological Active Compounds

Abstract

Compounds containing the coumarin scaffold are widely used in the pharmaceutical and medicinal industries. The biological activities of coumarin containing derivatives make the attractive for the develop new drugs. Different methods and techniques are developed to synthesize new drugs using coumarin as a starting material. This review summarized various methods, techniques and reaction conditions for synthesis of coumarins containing compounds from 3‐bromoacetylcoumarin. A total of 79 coumarin intermediates and products are reported herein. The different reactions include nucleophilic substitutions, one‐pot and multi‐step synthesis for preparation of coumarin containing compounds through different mechanisms and the outcomes achieved through such reactions are discussed. The prepared compounds showed a range of activities resulting in antifungal, antimicrobial, anti‐inflammatory, antidiabetic and cholinesterase inhibitors. The nucleophilic substitution reactions involving urea related compounds, followed by intramolecular cyclization lead to imidazole and thiazole moieties, which exhibit antibacterial activities. It is hoped that this review provides useful insight for researchers engaged in this field to expand the knowledge gained in this area.

Synthesis and discovery of potential tyrosinase inhibitor of new coumarin‐based thiophenyl‐pyrazolylthiazole nuclei: In vitro evaluation, cytotoxicity, kinetic, and computational studies

“…For developing high‐quality therapeutic candidates, we combined three heterocyclic units with a coumarin motif. Coumarin has attracted the attention of scientists due to its diverse biological activities in fields such as medicine, pharmacology, cosmetics, and the food industries (Hosseini Nasab, Azimian, et al, 2022; Nasab et al, 2022). Pyrazoline is another well‐known bioactive unit which has been reported to inhibit epidermal growth factor receptor tyrosine kinase (EGFR‐TK) (Lv et al, 2011), aurora kinase (Shin et al, 2013), COX‐2/B‐Raf (Yu et al, 2014), telomerase (Amin et al, 2015), and tubulin assembling (Qin et al, 2015).…”