Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists

Mohr, Florian; Hurrle, Thomas; Burggraaff, Lindsey; Langer, Lukas; Bemelmans, Martijn P.; Knab, Maximilian; Nieger, Martin; Heitman, Laura H.; Bräse, Stefan

doi:10.1016/j.ejmech.2021.113354

Cited by 1 publication

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“…Even if a significant activity of these compound against the CB1/CB2 receptors was not observed, this can be a starting point for further developments. Due to the involvement of ECS in numerous essential physiological and pathological processes, Bräse and co-workers evaluated the activity of different modified coumarins as cannabinoid receptor ligands ( Mohr et al, 2021 ). The most active compound, 180 , showed a CB2 selective agonistic profile ( K i = 6.5 nM, EC 50 = 4.51 nM, see Figure 1A ).…”

Section: Biological Applications Of Coumarin Derivativesmentioning

confidence: 99%

Syntheses, reactivity, and biological applications of coumarins

Citarella,

Vittorio,

Dank

et al. 2024

Front. Chem.

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This comprehensive review, covering 2021–2023, explores the multifaceted chemical and pharmacological potential of coumarins, emphasizing their significance as versatile natural derivatives in medicinal chemistry. The synthesis and functionalization of coumarins have advanced with innovative strategies. This enabled the incorporation of diverse functional fragments or the construction of supplementary cyclic architectures, thereby the biological and physico-chemical properties of the compounds obtained were enhanced. The unique chemical structure of coumarine facilitates binding to various targets through hydrophobic interactions pi-stacking, hydrogen bonding, and dipole-dipole interactions. Therefore, this important scaffold exhibits promising applications in uncountable fields of medicinal chemistry (e.g., neurodegenerative diseases, cancer, inflammation).

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Section: Biological Applications Of Coumarin Derivativesmentioning

confidence: 99%