1381763-25-2Relevant academic research and scientific papers
Gabapentin hybrid peptides and bioconjugates
Lebedyeva, Iryna O.,Ostrov, David A.,Neubert, John,Steel, Peter J.,Patel, Kunal,Sileno, Sean M.,Goncalves, Kevin,Ibrahim, Mohamed A.,Alamry, Khalid A.,Katritzky, Alan R.
, p. 1479 - 1486 (2014/03/21)
Synthetic approaches to gabapentin bioconjugates that overcome the tendency of gabapentin to cyclize into its γ-lactam are studied. Gabapentin was converted by N-acylation at its N-terminus into di-, tri-, and tetrapeptides (L-Ala-Gbp, L-Val-Gbp, L-Ala-L-Phe-Gbp, Gly-L-Ala-β-Ala-Gbp). Carboxyl-activated Boc-protected gabapentin was used to N-, O-, and S-acylate small peptides and hormones to give conjugates that could also provide prodrugs containing conformationally constrained gabapentin units.
