Author: Edwards, Sharon F. ; Chou, C. James ; Himes, Richard A. ; Prosser, Lyndsey C. ; Christie, Charleston F. ; Chan, Sherine S. L. ; West, Peter J. ; Metcalf, Cameron S. ; Watt, Emma ; Wilcox, Karen S. ; Li, Xiaoyang

Despite the availability of more than 25 antiseizure drugs on the market, approximately 30% of patients with epilepsy still suffer from seizures. Thus, the epilepsy therapy market has a great need for a breakthrough drug that will aid pharmacoresistant patients. In our previous study, we discovered a vitamin K analogue, 2h, which displayed modest antiseizure activity in zebrafish and mouse seizure models. However, there are limitations to this compound due to its pharmacokinetic profile. In this study, we develop a new series of vitamin K analogues by modifying the structure of 2h. Among these, compound 3d shows full protection in a rodent pharmacoresistant seizure model with limited rotarod motor toxicity and favorable pharmacokinetic properties. Furthermore, the brain/plasma concentration ratio of 3d indicates its excellent permeability into the brain. The resulting data shows that 3d can be further developed as a potential antiseizure drug in the clinic.

01 Nov 2019·Russian Journal of Organic Chemistry

Peculiarities of the Reaction of 2-Amino-1,4-naphthoquinones with 2,2-Dihydroxy-1H-indene-1,3(2H)-dione

Author: O. I. Fominykh ; Yu. G. Khalyavina ; L. M. Gornostaev ; Yu. V. Gatilov ; G. A. Stashina ; T. I. Lavrikova

The reaction of 2-amino-1,4-naphthoquinones with ninhydrin at 50-60°C in acetic acid leads to 4b,11b-dihydroxy-4b,5-dihydrobenzo[f]indeno[1,2-b]indole-6,11,12(11bH)-triones I [R = H, n-Pr, n-Bu, etc.; X = H, 8-OH].The products were isolated as hydrates and when heated in DMSO with methanesulfonic acid, they converted into 13-R-benzo[f]isochromeno[4,3-b]indole-5,7,12(13H)-triones II.

01 Jan 2016·Russian Journal of Organic Chemistry

Synthesis of 13-alkylbenzo[f]isochromeno[4,3-b]indole-5,7,12(13H)-triones by reaction of 2-alkylamino-1,4-naphthoquinones with ninhydrin

Author: Yu. G. Khalyavina ; D. A. Tropina ; O. I. Fominykh ; L. M. Gornostaev ; A. S. Kuznetsova ; I. A. Zamilatskov ; V. V. Chernyshev ; E. V. Murashova

Reactions of 2-alkylamino-1,4-naphthoquinones with 2,2-dihydroxy-1H-indene-1,3(2H)-dione afforded 13-alkylbenzo[f]isochromeno[4,3-b]indole-5,7,12(13H)-triones.

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Indication	Highest Phase	Country/Location	Organization	Date
Epilepsies, Myoclonic	Preclinical	United States	Neuroene Therapeutics LLC	-
Epilepsy	Preclinical	United States	The Medical University of South Carolina	-

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