247089-23-2Relevant academic research and scientific papers
Synthetic studies on CP-225,917 and CP-263,114: Access to advanced tetracyclic systems by intramolecular conjugate displacement and [2,3]-wittig rearrangement
Malihi, Farzad,Clive, Derrick L. J.,Chang, Che-Chien,Minaruzzaman
, p. 996 - 1013 (2013/04/10)
An advanced intermediate related to the structures of CP-225,917 and CP-263,114 was constructed by a sequence based on the use of Grob-like fragmentation, intramolecular conjugate displacement, and [2,3]-Wittig rearrangement. A variant of the [2,3]-Wittig rearrangement was developed.
Synthesis and characterization of novel bi- and tricyclic α-amino acids
Johnson, Matthew R.,Gauuan, Jolicia F.,Guo, Cheng,Guzzo, Peter R.,Le, Van-Duc,Shenoy, Rajesh A.,Hamby, James,Roark, Howard,Stier, Michael,Mangette, John E.
experimental part, p. 2769 - 2793 (2011/08/22)
As part of a medicinal chemistry collaboration, a number of novel bi- and tricyclic aamino acids were prepared through various routes and characterized by 1 H nuclearOverhauser effect difference experiments. The syntheses provide a number of routes to access some highly substituted amino acid derivatives that have not been reported previously. It is envisaged that the chemistry described here could be applied to the synthesis of other unique substrates Taylor & Francis Group, LLC.
Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase
Shankaran,Donnelly, Karla L.,Shah, Shrenik K.,Guthikonda, Ravindra N.,MacCoss, Malcolm,Humes, John L.,Pacholok, Stephen G.,Grant, Stephan K.,Kelly,Wong
, p. 4539 - 4544 (2007/10/03)
Syntheses and evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2- imines as inhibitors of nitric oxide synthase (NOS) are discussed. An extensive SAR was established for pyrrolidin-2-imines class of compounds. The amidines came out as the most potent inhibitors in addition to displaying selectivity.
Conformationally constrained amino acid compounds having affinity for the alpha2delta subunit of a calcium channel
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, (2008/06/13)
Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders
Synthesis and biological evaluation of conformationally restricted gabapentin analogues
Receveur, Jean-Marie,Bryans, Justin S.,Field, Mark J.,Singh, Lakhbir,Horwell, David C.
, p. 2329 - 2334 (2007/10/03)
A series of conformationally restricted Gabapentin analogues has been synthesised. The pyrrolidine analogue (R)-2-Aza-spiro[4.5]decane-4-carboxylic acid hydrochloride (3a) had an IC50 of 120nM, similar to that of Gabapentin (IC50 = 140nM), at the Gabapentin binding site on the α2δ subunit of a calcium channel. Compound (3a) also reversed carrageenan induced hyperalgesia in rats.
