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Historically, medicinal chemistry has been concerned with the approach of organic chemistry for new drug synthesis. Considering the fruitful collections of new molecular entities, the dedicated efforts for medicinal chemistry are rewarding. Planning and search for new and applicable pharmacologic therapies involve the altruistic nature of the scientists. Since the 19th century, notoriously applying isolated and characterized plant-derived compounds in modern drug discovery and various stages of clinical development highlight its viability and significance. Natural products influence a broad range of biological processes, covering transcription, translation, and post-translational modification, being effective modulators of most basic cellular processes. The research of new chemical entities through “click chemistry” continuously opens up a map for the remarkable exploration of chemical space towards leading natural products optimization by structure-activity relationship. Finally, in this review, we expect to gather a broad knowledge involving triazolic natural product derivatives, synthetic routes, structures, and their biological activities.

Coumarins (2H-chromen-2-ones) are heterocyclic compounds of wide scientific interest due to their important biological and pharmaceutical properties such as antitumor, antioxidant, anti-inflammatory and antimicrobial activities as well as enzymatic inhibitors related to neurodegenerative diseases. Due to their structural variability, this compound class has been attracting considerable interest in the natural products and synthetic organic chemistry areas. Coumarins and their derivatives have been prepared by a variety of methods, including Perkin, Wittig and Reformatsky reactions, Pechmann and Knoevenagel condensations, and Claisen rearrangement, among others. In the present review we report the different synthetic methods used in the preparation of coumarin derivatives exploited in the last ten years (from 2008 to 2018), regarding the research demand for new structural scaffolds.