Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 10, Pages 3644-3648Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0491795
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Funding
- NIDA NIH HHS [DA-04443] Funding Source: Medline
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On the basis of the structural features of the Dmt-Tic pharmacophore, a new motif leading to a fairly potent mu-opioid antagonist is described. This motif contains the 4-amino-1,2,4,5-tetrahydro-2-benzazepine-3-one skeleton as a substitute for the Tic residue, which provides the conformational constraint compatible with the mu-opioid receptor. The stereoselective synthesis of four stereoisomers is performed starting from homochiral 2',6'-dimethyltyrosine (Dmt) and o-aminomethylphenylalanine.
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