Analogues of (3 R)-7-Hydroxy-N-[(1 S)-1-{[(3 R, 4 R)-4-(3-hydroxyphenyl)-3, 4-dimethyl-1-piperidinyl] methyl}-2-methylpropyl)-1, 2, 3, 4-tetrahydro-3- …

SP Runyon, LE Brieaddy, SW Mascarella…

文献索引：Runyon, Scott P.; Brieaddy, Lawrence E.; Mascarella, S. Wayne; Thomas, James B.; Navarro, Hernan A.; Howard, James L.; Pollard, Gerald T.; Carroll, F. Ivy Journal of Medicinal Chemistry, 2010 , vol. 53, # 14 p. 5290 - 5301

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被引用次数: 17

摘要

The synthesis of compounds 6, 7a, b, 8a, b, 9a, b, and 10a, b where the amino− NH− group of JDTic (3) was replaced with an aromatic CH−, CH2, O, S, or SO group was accomplished and used to further characterize the SAR of the compound 3 class of κ opioid receptor antagonists. All of the compounds showed subnanomolar to low nanomolar K e values at the κ opioid receptor. The most potent compound was 7a, where the amino− NH ...