The Chromenopyrazole Scaffold in the Modulation of the Endocannabinoid System: A Broad Therapeutic Prospect

Paula Morales, Pilar Goya, Nadine Jagerovic


The endogenous cannabinoid system (ECS) has been recognized as one of the most important neuromodulatory systems. This system plays a crucial role in the regulation of numerous pathophysiological conditions such as pain, cancer, or neurodegeneration. Despite the vast effort focused on the development of drugs targeting the ECS, thus far, the clinical use of synthetic and phytogenic cannabinoids has been limited to pain, emesis and appetite due to their undesirable psychoactive properties. Therefore, novel strategies to therapeutically exploit the cannabinoids need to be developed to overcome these side-effects. Moreover, novel chemical tools to study the role of possible additional cannabinoid missing receptors, such as GPR55, need to be addressed to fully unravel the pharmacology of this complex system.

In this scenario, the chromenopyrazole scaffold was recently discovered as a privileged structure in drug discovery targeting the ECS. In this review, the development of novel modulators of the ECS based on the chromenopyrazole scaffold will be thoroughly discussed. Pharmacological avenues for this novel chemotype, as well as future perspectives will be analyzed.

Palabras clave

privileged scaffold; versatile; endocannabinoid system, cannabinoid receptors; GPR55; chromenopyrazole; drug design

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