Amino acid conjugates as kappa opioid receptor agonists.

Basic Information

ID: ALA1141989

Journal: Bioorg Med Chem Lett

Title: Amino acid conjugates as kappa opioid receptor agonists.

Authors: Kumar V, Guo D, Daubert JD, Cassel JA, DeHaven RN, Mansson E, DeHaven-Hudkins DL, Maycock AL.

Abstract: A novel series of kappa (kappa) opioid receptor agonists were synthesized by incorporating the key structural features of known kappa opioid agonists while replacing the aryl acetamide portion with substituted amino acid conjugates. Compounds 3j (Ki = 6.7 nM), 3k (Ki = 3.6 nM), 3l (Ki = 4.6 nM), 3m (Ki = 0.83 nM) and 3o (Ki = 2 nM) possessed potent affinities for the kappa opioid receptor in vitro with reasonable selectivity over other opioid receptors.

CiteXplore: 15713370

DOI: 10.1016/j.bmcl.2005.01.038

Patent ID: