β-Analogs of PLG (l-prolyl-l-leucyl-glycinamide): Ex-chiral pool syntheses and dopamine D2 receptor modulating effects
摘要:
Starting from (S)- and (R)-aspartic acid enantiomerically pure P-proline derivatives were synthesized. These chiral building blocks were transformed into P-analogs of the dopamine receptor modulating peptide PLG. According to dopamine receptor binding studies, significant enhancement of [H-3]pramipexole binding was observed for the isomeres 1a,b and 2a-c. The derivative Ib revealed an activity comparable to PLG. (C) 1998 Elsevier Science Ltd. Air rights reserved.
β-Analogs of PLG (l-prolyl-l-leucyl-glycinamide): Ex-chiral pool syntheses and dopamine D2 receptor modulating effects
摘要:
Starting from (S)- and (R)-aspartic acid enantiomerically pure P-proline derivatives were synthesized. These chiral building blocks were transformed into P-analogs of the dopamine receptor modulating peptide PLG. According to dopamine receptor binding studies, significant enhancement of [H-3]pramipexole binding was observed for the isomeres 1a,b and 2a-c. The derivative Ib revealed an activity comparable to PLG. (C) 1998 Elsevier Science Ltd. Air rights reserved.