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Bioorg Med Chem Lett. 2006 May 1;16(9):2505-8. Epub 2006 Feb 17.

Identification of potent phenyl imidazoles as opioid receptor agonists.

Author information

1
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Welsh and McKean Roads, PO Box 776, Spring House, PA 19477-0776, USA. HBreslin@prdus.jnj.com

Abstract

Using previously reported opioid receptor (OR) agonist analogs 4a-c as starting points, the structure-activity relationship (SAR) for their related series has been further refined. This SAR study has led to the identification of 2,6-di-Me-Tyr (DMT) analogs 4h and 4j as the most potent OR agonist within the series. In addition, it was discovered that 4-(aminocarbonyl)-2,6-dimethyl-Phe is a reasonable bioisostere surrogate for the DMT moiety, as supported by the OR activities of compounds 4x and 4y.

PMID:
16483774
DOI:
10.1016/j.bmcl.2006.01.082
[Indexed for MEDLINE]

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