Synthesis of Pro-Leu-Gly-NH2Analogues Modified at the Prolyl Residue and Evaluation of Their Effects on the Receptor Binding Activity of the Central Dopamine Receptor Agonist, ADTN

Rodney L Johnson, Kuo Long Yu, G. Rajakumar, Ram K. Mishra

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Abstract

Several analogues of L-prolyl-L-leucylglycinamide (PLG) were synthesized wherein the prolyl residue was replaced with other heterocyclic amino acid residues. Among the analogues synthesized were D-Pro-Leu-Gly-NH2(2), <Glu-Leu-Gly-NH2(3), Thz-Leu-Gly-NH2(4), Pip-Leu-Gly-NH2(5), Aze-Leu-Gly-NH2(6), L-Δ34-Pro-Leu-Gly-NH2(7), and D-Δ3,4-Pro-Leu-Gly-NH2(8). These analogues were tested for their ability to enhance the binding of the agonist 2-amino-6,7-dihydroxy-l,2,3,4-tetrahydronaphthalene to central dopamine receptors. Analogues 2, 3, and 5–7 showed activity comparable to that of PLG, while the tripeptides 4 and 8 were found to be inactive. The results show that the N-terminal prolyl residue of PLG is not an essential requirement for this tripeptide's ability to modulate dopamine receptors.

Original languageEnglish (US)
Pages (from-to)2104-2107
Number of pages4
JournalJournal of medicinal chemistry
Volume29
Issue number10
DOIs
StatePublished - 1986

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