106076-00-0Relevant academic research and scientific papers
Novel l-prolyl-l-leucylglycinamide (PLG) tripeptidomimetics based on a 2-azanorbornane scaffold as positive allosteric modulators of the D2R
Sampaio-Dias, Ivo E.,Sousa, Carlos A. D.,García-Mera, Xerardo,Ferreira Da Costa, Joana,Caama?o, Olga,Rodríguez-Borges, José E.
supporting information, p. 11065 - 11069 (2016/12/09)
An efficient and straightforward orthogonal methodology was successfully developed to achieve constrained l-prolyl-l-leucylglycinamide (PLG) analogues starting from two proline mimetics based on a 2-azanorbornane scaffold. A preliminary dopamine D2 receptor radiolabeled binding assay with [3H]-N-propylnorapomorphine shows that enantiopurity of PLG peptidomimetics based on 2-azanorbornane is a requirement to achieve statistically significant positive modulators of the D2 receptor. This is the first documented active peptidomimetic of PLG whose bioactivity is not correlated with the C-terminal carboxamide pharmacophore and which cannot adopt the hypothesized type II β-turn conformation.
AZA DIELS-ALDER REACTIONS IN WATER: CYCLOCONDENSATION OF C-ACYL IMINIUM IONS WITH CYCLOPENTADIENE
Grieco, Paul A.,Larsen, Scott D.,Fobare, William F.
, p. 1975 - 1978 (2007/10/02)
C-Acyl N-alkyl iminium ions as well as C-acyl N-unsubstituted iminium ions react with cyclopentadiene in water at ambient temperature giving rise to aza Diels-Alder adducts.
