Review on the Synthetic Methods of Biologically Potent Benzoxazole Derivatives

Abstract

Abstract:: Benzoxazole compounds have an important and broad range of biological activities. The benzoxazole and its substituted derivatives possess antimicrobial, antitumor, anti-inflammatory, antihistaminic, anti-parasitic, herbicidal, antiallergic, anti-helmintic, anti-tubercular, anticonvulsant, hypoglycaemic, HIV-1 reverse transcriptase inhibitor and insecticidal activities. It has also been shown to have binding affinity to Aβ42 fibrils. Such complex biological uses of benzoxazole compounds have inspired new efforts to find new derivatives with improved biological activity and different applications in the pharmaceutical industry. Outstanding the relevance of this structure, the purpose of this analysis is to highlight aspects published in recent years (2000-2020) on the chemistry and biological activity of benzoxazoles.

Design, synthesis, and cytotoxicity of ibuprofen-appended benzoxazole analogues against human breast adenocarcinoma

“…Heterocyclic molecules containing oxygen and nitrogen atoms have gained prominence due to their varied pharmacological activities. 23–25 Benzoxazole is one of the most important heterocyclic compounds that exhibit remarkable pharmacological activities 26 such as anticancer, 27 anthelmintic, 28 cyclooxygenase inhibitory, 29 antifungal, 30 antitubercular, 31 5HT3 receptor antagonists, 32 antiinflammatory, 33 analgesic 34 and cyclin-dependent kinase inhibitory, 35 5-lipoxygenase inhibitory, 36 melatonin receptor agonist, 37 antibacterial, 38 antiHIV, 39 anticonvulsant, 40 antiviral, 41 antiallergic, 42 cyclooxygenase 2 (COX-2) inhibitory, 43 antihyperglycemic, 44 dopamine D4 agonists, 43 herbicidal, 45 amyloidogenesis inhibitors, 46 rho kinase inhibitors, 47 and diarrhea-dependent irritable bowel syndrome property. 48 Other than biology, benzoxazoles have various applications such as fluorescent, 49 brighteners, 50 whitening agents, 51 ballistic materials, 52 and sensors.…”

Biomedical applications of selective metal complexes of indole, benzimidazole, benzothiazole and benzoxazole: A review (From 2015 to 2022)

“…Many benzoxazole derivatives have been produced and tested for their biological potential, which showed significant antimicrobial, antitumor, anti-inflammatory, anti-histaminic, anti-parasitic, anti-allergic, anthelmintic, anti-tubercular, anticonvulsant, hypoglycemic, and antiviral potency. ( Arulmurugan et al, 2020 , Wong and Yeong, 2021 ) The benzoxazole derivatives have been also reported for the fluorescent and colorimetric sensor for the recognition of different pollutants which is an emerging attractive area of particular interest in chemical biology and analytical chemistry ( Xu et al, 2014 , Yang et al, 2016 ). Furthermore, the metal complexes of these compounds also showed excellent biological and catalytic activities ( Balaghi et al, 2013 , Sun et al, 2022 ).…”