A Patent Review on the Current Developments of Benzoxazoles in Drug Discovery

Abstract

medicinal aspects of patented benzoxazole derivatives are discussed. The recent development and drawbacks are also reviewed.

Alternative Benzoxazole Assembly Discovered in Anaerobic Bacteria Provides Access to Privileged Heterocyclic Scaffold

“…[1] As a nucleotide bioisoster, the benzoxazole scaffold is privileged for binding to various targets and biopolymers. [2] One medicinally used benzoxazole derivative is tafamidis (1), which delays neurodegeneration and other severe diseases linked to transthyretin amyloidosis. [3] Moreover, numerous benzoxazole derivatives have been explored as leads for development of antituberculosis (2) [4] or anti-inflammatory drugs (3, 4).…”

“…Owing to their broad range of biological activities, benzoxazoles are among the most prominent classes of pharmaceutically relevant heterocycles [1] . As a nucleotide bioisoster, the benzoxazole scaffold is privileged for binding to various targets and biopolymers [2] .…”

Iodine-catalyzed synthesis of benzoxazoles using catechols, ammonium acetate, and alkenes/alkynes/ketones via C–C and C–O bond cleavage

“…[5][6][7][8] Benzoxazoles are one of the important classes of nitrogen-containing heterocycles with extensive utilization especially in medicinal chemistry. 9,10 Moreover, the benzoxazole heterocycle is one of the widely found structures in nature, and a range of related natural products are known as potent pharmacophores (Fig. 1).…”

Silver Ions Promoted Palladium-Catalyzed Inactive β-C(sp3)–H Bond Arylation in Batch and Continuous-Flow Conditions

“…A variety of heterocyclic substrates have been identified as potential activators of inactive C–H bonds . In this context, nitrogen-containing heterocycles such as benzothiazoles, benzimidazoles, and benzoxazoles are the ubiquitous feature of bioactive natural products and versatile structural motifs that could be found in various pharmaceuticals and synthetic materials …”