247089-07-2Relevant 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
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.
