Heterocyclic compounds are found in nature and exhibit important biological activities. Isoquinolines are one such class of heterocycles with applications in many fields including materials science, pharmaceuticals, and agrochemicals. Important naturally occurring isoquinolines are papaverine, sanguinarine, berberine, and coptisine. They act as an essential part of the chemical defense system in many plants and fend off herbivores. Berberine exhibits diverse pharmacological effects such as analgesic, anti-inflammatory, antitumor, antimicrobial, blood pressure-lowering, and hypolipidemic activities. Inspired by nature, many clinical drugs containing the isoquinoline core are being developed. This review summarizes the pharmacological activities, mode of action and chemical synthesis of approved clinical drugs containing isoquinoline core.
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