103790-23-4Relevant academic research and scientific papers
NMDA RECEPTOR ANTAGONISTS FOR NEUROPROTECTION
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, (2021/03/18)
Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurode
Synthesis, structural activity-relationships, and biological evaluation of novel amide-based allosteric binding site antagonists in NR1A/NR2B N-methyl-d-aspartate receptors
Mosley, Cara A.,Myers, Scott J.,Murray, Ernest E.,Santangelo, Rose,Tahirovic, Yesim A.,Kurtkaya, Natalie,Mullasseril, Praseeda,Yuan, Hongjie,Lyuboslavsky, Polina,Le, Phuong,Wilson, Lawrence J.,Yepes, Manuel,Dingledine, Ray,Traynelis, Stephen F.,Liotta, Dennis C.
, p. 6463 - 6480 (2011/03/17)
The synthesis and structure-activity relationship analysis of a novel class of amide-based biaryl NR2B-selective NMDA receptor antagonists are presented. Some of the studied compounds are potent, selective, non-competitive, and voltage-independent antagonists of NR2B-containing NMDA receptors. Like the founding member of this class of antagonists (ifenprodil), several interesting compounds of the series bind to the amino terminal domain of the NR2B subunit to inhibit function. Analogue potency is modulated by linker length, flexibility, and hydrogen bonding opportunities. However, unlike previously described classes of NR2B-selective NMDA antagonists that exhibit off-target activity at a variety of monoamine receptors, the compounds described herein show much diminished effects against the hERG channel and α1-adrenergic receptors. Selections of the compounds discussed have acceptable half-lives in vivo and are predicted to permeate the blood-brain barrier. These data together suggest that masking charged atoms on the linker region of NR2B-selective antagonists can decrease undesirable side effects while still maintaining on-target potency.
Antiarrhythmic N-aminoalkylene alkyl and aryl sulfonamides
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, (2008/06/13)
The present invention provides novel sulfonanilide and benzene-alkylaminium compounds which are the products of processes utilizing novel intermediates. Both the novel compounds and the novel intermediates are useful for the therapeutic or prophylactic treatment of arrhythmic activity.
Spirodienones. Part 5. The Synthesis and Reactions of N-Sulphonylcyclohexadienimines
Coutts, Ian G. C.,Culbert, Nicholas J.,Edwards, Mark,Hadfield, John A.,Musto, Donald R.,et al.
, p. 1829 - 1836 (2007/10/02)
The anodic or chemical oxidation of para-substituted sulphonanilides gives 4,4-disubstituted N-sulphonylcyclohexadienimines, which, from appropriately substituted anilines, may be spirocyclic.The scope and limitations of the synthesis are described, and mechanism proposed.The selective hydrolysis of the dienimines to the corresponding dienones provides a convenient route to the latter compounds.The reaction of some of the dienimines with dienes is discussed.
