247089-12-9Relevant academic research and scientific papers
Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors
Bondada, Lavanya,Rondla, Ramu,Pradere, Ugo,Liu, Peng,Li, Chengwei,Bobeck, Drew,McBrayer, Tamara,Tharnish, Philip,Courcambeck, Jerome,Halfon, Philippe,Whitaker, Tony,Amblard, Franck,Coats, Steven J.,Schinazi, Raymond F.
, p. 6325 - 6330 (2013/11/19)
Herein, we report the synthesis and structure-activity relationship studies of new analogs of boceprevir 1 and telaprevir 2. Introduction of azetidine and spiroazetidines as a P2 substituent that replaced the pyrrolidine moiety of 1 and 2 led to the disco
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.
