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Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profile.
Kormos CM, Gichinga MG, Maitra R, Runyon SP, Thomas JB, Brieaddy LE, Mascarella SW, Navarro HA, Carroll FI. Kormos CM, et al. J Med Chem. 2014 Sep 11;57(17):7367-81. doi: 10.1021/jm5008177. Epub 2014 Aug 25. J Med Chem. 2014. PMID: 25133923 Free PMC article.
Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)- N-[1 R)-1-(Cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (CDTic).
Kormos CM, Ondachi PW, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Fennell TR, Snyder RW, Carroll FI. Kormos CM, et al. J Med Chem. 2018 Sep 13;61(17):7546-7559. doi: 10.1021/acs.jmedchem.8b00674. Epub 2018 Aug 29. J Med Chem. 2018. PMID: 30032602 Free PMC article.
Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3 R)-7-Hydroxy- N-[(1 S)-2-methyl-1-(piperidin-1-ylmethyl)propyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (PDTic).
Ondachi PW, Kormos CM, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Fennell TR, Snyder RW, Carroll FI. Ondachi PW, et al. Among authors: kormos cm. J Med Chem. 2018 Sep 13;61(17):7525-7545. doi: 10.1021/acs.jmedchem.8b00673. Epub 2018 Aug 29. J Med Chem. 2018. PMID: 30117738 Free PMC article.
20 results