TY - JOUR
T1 - trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines
T2 - A novel class of μ-Selective opioid antagonists
AU - Le Bourdonnec, Bertrand
AU - Belanger, Serge
AU - Cassel, Joel A.
AU - Stabley, Gabriel J.
AU - DeHaven, Robert N.
AU - Dolle, Roland E.
PY - 2003/12/15
Y1 - 2003/12/15
N2 - trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines constitute a novel class of μ opioid receptor antagonists. The CONH2 group was found to be an effective isostere of the phenolic OH moiety. Structure-activity relationships at the piperidine nitrogen position led to the identification of several ligands displaying high affinity toward the cloned human μ opioid receptors, good selectivity μ/δ, μ/κ, and potent in vitro antagonist activity.
AB - trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines constitute a novel class of μ opioid receptor antagonists. The CONH2 group was found to be an effective isostere of the phenolic OH moiety. Structure-activity relationships at the piperidine nitrogen position led to the identification of several ligands displaying high affinity toward the cloned human μ opioid receptors, good selectivity μ/δ, μ/κ, and potent in vitro antagonist activity.
UR - http://www.scopus.com/inward/record.url?scp=0344308940&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2003.09.012
DO - 10.1016/j.bmcl.2003.09.012
M3 - Article
C2 - 14643346
AN - SCOPUS:0344308940
SN - 0960-894X
VL - 13
SP - 4459
EP - 4462
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 24
ER -