99972-91-5Relevant articles and documents
Highly Active Manganese to C?O Cross-Coupling Reaction for the Synthesis of N-Hydroxyphthalimide Esters
Joo, Seong-Ryu,Kim, Jong-Sung,Park, Soo-Youl,Kim, Seung-Hoi
, p. 829 - 832 (2018/04/30)
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Synthesis and evaluation of potent KCNQ2/3-specific channel activators
Kumar, Manoj,Reed, Nicholas,Liu, Ruiting,Aizenman, Elias,Wipf, Peter,Tzounopoulos, Thanos
supporting information, p. 667 - 677 (2016/07/06)
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.
Synthesis and Anticonvulsant Activity of Imidooxy Derivatives
Edafiogho, Ivan O.,Scott, K. R.,Moore, Jacqueline A.,Farrar, Vida A.,Nicholson, Jesse M.
, p. 387 - 392 (2007/10/02)
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