99972-91-5

Upstream product

• 541-41-3 chloroformic acid ethyl ester 
• 70206-52-9 sodium salt of 2-hydroxy-1H-isoindole-1,3(2H)-dione 
• 524-38-9 N-hydroxyphthalimide 
• 64-17-5 ethanol 
• 78816-91-8 bis(1,3-dioxoisoindolin-2-yl)carbonate 

Relevant academic research and scientific papers

(2-AMINO-4(ARYLAMINO)PHENYL) CARBAMATES

A compound, or pharmaceutically acceptable salt thereof, having a formula (I) wherein R1 is H or optionally-substituted alkyl; R2 is optionally-substituted alkyl; R3 and R4 are each independently H or optionally-substituted alkyl; R5 is H, optionally-substituted alkyl, acyl, or alkoxycarbonyl; R6 and R7 are each independently H, deuterium, optionally- substituted alkyl, or R6 and R7 together form a carbocyclic; R8 is optionally-substituted thiazolyl, optionally-substituted thiophenyl, or substituted phenyl, provided that if R8 is 4-halophenyl, then R2 is substituted alkyl or branched alkyl or at least one of R6 or R7 is not H; and R30, R31 and R32 are each independently H, deuterium, halogen, substituted sulfanyl, or optionally-substituted alkoxy.

Synthesis and evaluation of potent KCNQ2/3-specific channel activators

KQT-like subfamily (KCNQ) channels are voltage-gated, non-inactivating potassium ion channels, and their down-regulation has been implicated in several hyperexcitability-related disorders, including epilepsy, neuropathic pain, and tinnitus. Activators of these channels reduce the excitability of central and peripheral neurons, and, as such, have therapeutic utility. Here, we synthetically modified several moieties of the KCNQ2-5 channel activator retigabine, an anticonvulsant approved by the U.S. Food and Drug Administration. By introducing a CF3-group at the 4-position of the benzylamine moiety, combined with a fluorine atom at the 3-position of the aniline ring, we generated Ethyl (2-amino-3-fluoro-4-((4-(trifluoromethyl)benzyl)amino)phenyl)carbamate (RL648-81), a new KCNQ2/3-specific activator that is >15 times more potent and also more selective than retigabine. We suggest that RL648-81 is a promising clinical candidate for treating or preventing neurologic disorders associated with neuronal hyperexcitability.

Carbethoxylating Agents as Inhibitors of Aldehyde Dehydrogenase

N,O-Dicarbethoxy-4-chlorobenzenesulfohydroxamate (1c) and O-carbethoxy-N-hydroxysaccharin (6), both potential carbethoxylating agents, inhibited yeast aldehyde dehydrogenase (AlDH) with IC50's of 24 and 56 μM, respectively.The esterase activity of the enz

Synthesis and Anticonvulsant Activity of Imidooxy Derivatives

Previous results of anticonvulsant activity in several imidooxy carboxylates related to (aminooxy)acetic acid in young chicks, prompted an in-depth reinvestigation of these analogues in mice.A series of 22 succinimidooxy, phthalimidooxy, and naphthalimido