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Bioorg Med Chem Lett. 2002 Nov 4;12(21):3175-8.

Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.

Author information

1
Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA.

Abstract

Modulation of opioid activity was accomplished for analogues of Leu-enkephalin through incorporation of a 4-imidazolidinone moiety. The peptide backbone was constrained via a methylene bridge between two neighboring amides within its regular peptide sequence, which was expected to disrupt the secondary structure of the original molecule. Five positional analogues of Leu-enkephalin based on the same sequence and different location of the imidazolidinone-constrict were designed, synthesized, and examined for their affinity to micro-, delta- and kappa-opioid receptors.

PMID:
12372527
DOI:
10.1016/s0960-894x(02)00678-9
[Indexed for MEDLINE]

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