Porter, JD; Vivas, O; Weaver, CD; Alsafran, A; DiMilo, E; Arnold, LA; Dickson, EJ; Dockendorff, C in [Porter, Jacob D.; Alsafran, Abdulmohsen; Dockendorff, Chris] Marquette Univ, Dept Chem, POB 1881, Milwaukee, WI 53201 USA; [Vivas, Oscar; Dickson, Eamonn J.] Univ Calif Davis, Dept Physiol & Membrane Biol, 1 Shields Ave, Davis, CA 95616 USA; [Weaver, C. David] Vanderbilt Univ, Vanderbilt Inst Chem Biol, Dept Pharmacol, Nashville, TN 37232 USA; [Weaver, C. David] Vanderbilt Univ, Vanderbilt Inst Chem Biol, Dept Chem, Nashville, TN 37232 USA; [DiMilo, Elliot; Arnold, Leggy A.] Univ Wisconsin, Milwaukee Inst Drug Discovery, Dept Chem & Biochem, Milwaukee, WI 53211 USA published An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders in 2019, Cited 34. Recommanded Product: Anthrone. The Name is Anthrone. Through research, I have a further understanding and discovery of 90-44-8.
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 (compound 18, JDP-107) with a promising combination of potency (IC50=0.16 mu M 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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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem