Chemical Development of MDL 103371:  An <i>N</i>-Methyl-<scp>d</scp>-Aspartate-Type Glycine Receptor Antagonist for the Treatment of Stroke

Watson, Timothy; Horgan, S. W.; Shah, Ramnik S.; Farr, Robert A.; Schnettler, Richard A.; Nevill, C. Richard; Weiberth, Franz J.; Huber, Edward W.; Baron, Bruce M.; Webster, Mark E.; Mishra, Rajesh; Harrison, Boyd L.; Nyce, Phillip; Rand, and Cynthia L.; Goralski, Christian T.

doi:10.1021/op000286s

Cited by 33 publications

(14 citation statements)

References 20 publications

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“…Optimized yields and selectivities for a variety of “real world” substrates in the presence of several other functional groups can be very high, but it has to be stressed that this is not always the case 54. An interesting result was reported for the hydrogenation of a complex nitroarene intermediate with a cyanovinyl moiety whereby a Rh/Al 2 O 3 catalyst in the presence of NEt 3 achieved excellent results 56…”

Section: Assessment Of Catalytic Systems For Selected Selectivity Promentioning

confidence: 99%

Selective Catalytic Hydrogenation of Functionalized Nitroarenes: An Update

Blaser¹,

Steiner²,

2009

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Section: Assessment Of Catalytic Systems For Selected Selectivity Promentioning

confidence: 99%

Selective Catalytic Hydrogenation of Functionalized Nitroarenes: An Update

Blaser¹,

Steiner²,

2009

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“…[xlviii] 2,3-Disubtituted indoles can be found in a number of therapeutic agents of serious diseases such as developmental disorders, stroke, and hypercholesterolemia. [xlix] …”

Section: Sequential Larock Indole Synthesis/cross-couplingmentioning

confidence: 99%

Sequential Processes in Palladium‐Catalyzed Silicon‐Based Cross‐Coupling

Denmark

Liu

2010

Israel Journal of Chemistry

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Although developed somewhat later, silicon-based cross-coupling has become a viable alternative to the more conventional Suzuki-Miyaura, Stille-Kosugi-Migita, and Negishi cross-coupling reactions because of its broad substrate scope, high stability of silicon-containing reagents, and low toxicity of waste streams. An empowering and yet underappreciated feature unique to silicon-based cross-coupling is the wide range of sequential processes available. In these processes, simple precursors are first converted to complex silicon-containing cross-coupling substrates, and the subsequent silicon-based cross-coupling reaction affords an even more highly functionalized product in a stereoselective fashion. In so doing, structurally simple and inexpensive starting materials are quickly transformed into value-added and densely substituted products. Therefore, sequential processes are often useful in constructing the carbon backbones of natural products. In this review, studies of sequential processes involving silicon-based cross-coupling are discussed. Additionally, the total syntheses that utilize these sequential processes are also presented.

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“…Activity resides exclusively in the E isomer. MDL-103,371 provided protection against convulsions in different seizure models [39,40].…”

Section: Indole-2-carboxylic Acids and Tricy-clic Derivativesmentioning

confidence: 99%

Competitive Gly/NMDA Receptor Antagonists

Catarzi¹,

Colotta²,

Varano

2006

CTMC

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Glutamic acid (Glu) is the major excitatory neurotransmitter in the mammalian central nervous system (CNS) where it is involved in the physiological regulation of different processes. It has been well established that excessive endogenous Glu is associated with many acute and chronic neurodegenerative disorders such as cerebral ischemia, epilepsy, amiotrophic lateral sclerosis (ALS), Parkinson's and Alzheimer's diseases. In addition to the classical competitive glutamate receptor (GluR) antagonists, much effort has been directed toward the development of many different non-competitive antagonists of these receptors and, among them, compounds blocking the glycine site on the NMDA receptor complex (Gly/NMDA) have been widely investigated. Many Gly/NMDA receptor antagonists showed to be potential therapeutic agents in many neurological diseases such as stroke, epilepsy and neuropathic pain. Some of them, endowed also with favourable physicochemical properties and low secondary undesiderable effects, reached clinical trials.

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Chemical Development of MDL 103371: An N-Methyl-d-Aspartate-Type Glycine Receptor Antagonist for the Treatment of Stroke

Cited by 33 publications

References 20 publications

Selective Catalytic Hydrogenation of Functionalized Nitroarenes: An Update

Selective Catalytic Hydrogenation of Functionalized Nitroarenes: An Update

Sequential Processes in Palladium‐Catalyzed Silicon‐Based Cross‐Coupling

Competitive Gly/NMDA Receptor Antagonists

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