Equipower and Equichordal Extension

Stępnicki, R.

doi:10.1515/dema-2004-0414

Demonstratio Mathematica

2004

DOI: 10.1515/dema-2004-0414

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Equipower and Equichordal Extension

R. Stępnicki¹

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2019

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“…targets. [1][2][3] One approach to schizophrenia drug discovery involves the repurposing of compounds that have at least demonstrated safety in clinical trials. 4 With this in mind, our interest in the chemical modification and redesign of bioactive natural and unnatural scaffolds led us to reexamine blockers of specific voltage-gated potassium channels of the family Kv7 (KCNQ).…”

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confidence: 99%

An Anthrone-Based Kv7.2/7.3 Channel Blocker with Improved Properties for the Investigation of Psychiatric and Neurodegenerative Disorders

Porter¹,

Vivas-Rodriguez²,

Weaver³

et al. 2019

Preprint

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A set of novel Kv7.2/7.3 (KCNQ2/3) channel blockers was synthesized to address several liabilities of the known compounds XE991 (metabolic instability and CYP inhibition) and the clinical compound DMP 543 (acid instability, insolubility, and lipophilicity). Using the anthrone scaffold of the prior channel blockers, alternative heteroarylmethyl substituents were installed via enolate alkylation reactions. Incorporation of a pyridazine and a fluorinated pyridine gave an analog (JDP-107) with an optimal combination of potency (IC<sub>50</sub>= 0.16 𝜇M in a Kv7.2 thallium flux assay), efficacy in a Kv7.2/7.3 patch clamp assay, and drug-like properties.

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mentioning

confidence: 99%

An Anthrone-Based Kv7.2/7.3 Channel Blocker with Improved Properties for the Investigation of Psychiatric and Neurodegenerative Disorders

Porter¹,

Vivas-Rodriguez²,

Weaver³

et al. 2019

Preprint

View full text Add to dashboard Cite

show abstract

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Equipower and Equichordal Extension

Cited by 1 publication

References 5 publications

An Anthrone-Based Kv7.2/7.3 Channel Blocker with Improved Properties for the Investigation of Psychiatric and Neurodegenerative Disorders

An Anthrone-Based Kv7.2/7.3 Channel Blocker with Improved Properties for the Investigation of Psychiatric and Neurodegenerative Disorders

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