Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache

Blanco, Marı́a-Jesús; Benesh, Dana R.; Knobelsdorf, J.; Khilevich, Albert; Cortez, Guillermo S.; Mokube, Fese; Aicher, Thomas D.; Groendyke, Todd M.; Marmsater, Fredrik; Tang, Tony P.; Johnson, Kirk W.; Clemens‐Smith, Amy; Muhlhauser, Mark; Swanson, Steven; Catlow, John T.; Emkey, Renee; Johnson, Michael P.; Schkeryantz, Jeffrey M.

doi:10.1016/j.bmcl.2016.11.049

Cited by 5 publications

(2 citation statements)

References 29 publications

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“…Moreover, it also possessed significant antagonist potency against cysteinyl leukotriene receptor 1 (its antagonist is considered as an approach for preventing and treating recurrent primary headaches). The outcomes of further in vivo assays showed that compound 113 exhibited a full therapeutic effect in the migraine rat model . The design of this multitarget compound with 113 as an example would provide a feasible approach to develop more effective agents for treating migraine headaches.…”

Section: Application Of De Scaffold In Medicinal Chemistrymentioning

confidence: 99%

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Diaryl Ether: A Privileged Scaffold for Drug and Agrochemical Discovery

Chen

Xiong

Yang

et al. 2020

J. Agric. Food Chem.

100

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Diaryl ether (DE) is a functional scaffold existing widely both in natural products (NPs) and synthetic organic compounds. Statistically, DE is the second most popular and enduring scaffold within the numerous medicinal chemistry and agrochemical reports. Given its unique physicochemical properties and potential biological activities, DE nucleus is recognized as a fundamental element of medicinal and agrochemical agents aimed at different biological targets. Its drug-like derivatives have been extensively synthesized with interesting biological features including anticancer, anti-inflammatory, antiviral, antibacterial, antimalarial, herbicidal, fungicidal, insecticidal, and so on. In this review, we highlight the medicinal and agrochemical versatility of the DE motif according to the published information in the past decade and comprehensively give a summary of the target recognition, structure–activity relationship (SAR), and mechanism of action of its analogues. It is expected that this profile may provide valuable guidance for the discovery of new active ingredients both in drug and pesticide research.

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Section: Application Of De Scaffold In Medicinal Chemistrymentioning

confidence: 99%

“…The outcomes of further in vivo assays showed that compound 113 exhibited a full therapeutic effect in the migraine rat model. 148 The design of this multitarget compound with 113 as an example would provide a feasible approach to develop more effective agents for treating migraine headaches.…”

Section: ■ Introductionmentioning

confidence: 99%