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Published on: December 1, 2020
Oxazole and isoxazole-containing pharmaceuticals: targets, pharmacological activities, and their SAR studies
Shanshan Li1, Yiou Mei1, Luchen Jiang1
1Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Faculty of Medicine, Tianjin University Tianjin 300072 China duyunfeier@tju.edu.cn +86 22 27406121.
Abstract:
Oxazole, a five-membered aromatic heterocycle featuring a nitrogen and an oxygen atom separated by a carbon atom, and its isomer isoxazole, with directly attached oxygen and nitrogen atoms, have been pivotal in medicinal chemistry. Over the past few decades, the U.S. Food and Drug Administration (FDA) has approved more than 20 drugs containing these nuclei for various clinical conditions, including Tafamidis and Oxaprozin. Due to their unique physicochemical properties, these drugs often exhibit superior pharmacokinetic profiles and pharmacological effects compared to those with similar heterocycles. This review provides a comprehensive overview of all FDA-approved drugs containing oxazole and isoxazole nuclei, focusing on their pharmacological activities and structure-activity relationships.
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