COCAINE RECEPTOR BINDING LIGANDS

摘要

Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have formula (I), wherein Y = CH2R3, CO2R2 or (II), R1 = hydrogen, C1-5 alkyl, R2 = hydrogen, C1-6 alkyl, C3-8 cycloalkyl, C1-4 alkoxy, C1-6 alkynyl, halogen or amine, R3 = OH, hydrogen, C1-6 alkyl, C3-8 cycloalkyl, C1-4 alkoxy, Cl, Br, I, CN, NH2, NHC1-6 alkyl, NC1-6 alkyl, OCOC1-6 alkyl, OCOC1-3 alkylaryl, A = S, O or NH, X = H, C1-6 alkyl, C3-8 cycloalkyl, C1-4 alkoxy, C1-6 alkynyl, halogen, amino, acylamido, and Z = H, I, Br, C1, F, CN, CF3 NO2, N3, OR1, CO2NH2, CO2R1, C1-6 alkyl, NR4R5, NHCOR5, NHCO2R6, wherein R4-R6 are each C1-6 alkyl.