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Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.
Runyon SP, Brieaddy LE, Mascarella SW, Thomas JB, Navarro HA, Howard JL, Pollard GT, Carroll FI. Runyon SP, et al. Among authors: thomas jb. J Med Chem. 2010 Jul 22;53(14):5290-301. doi: 10.1021/jm1004978. J Med Chem. 2010. PMID: 20568781 Free PMC article.
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. Among authors: thomas jb. 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.
Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
Thomas JB, Giddings AM, Wiethe RW, Olepu S, Warner KR, Sarret P, Gendron L, Longpre JM, Zhang Y, Runyon SP, Gilmour BP. Thomas JB, et al. J Med Chem. 2014 Sep 11;57(17):7472-7. doi: 10.1021/jm500857r. Epub 2014 Aug 26. J Med Chem. 2014. PMID: 25157640 Free PMC article.
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
Thomas JB, Giddings AM, Olepu S, Wiethe RW, Harris DL, Narayanan S, Warner KR, Sarret P, Longpre JM, Runyon SP, Gilmour BP. Thomas JB, et al. Bioorg Med Chem Lett. 2015 Jan 15;25(2):292-6. doi: 10.1016/j.bmcl.2014.11.047. Epub 2014 Nov 24. Bioorg Med Chem Lett. 2015. PMID: 25499438 Free PMC article.
Identification of 2-({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)tricyclo[3.3.1.13,7]decane-2-carboxylic Acid (NTRC-844) as a Selective Antagonist for the Rat Neurotensin Receptor Type 2.
Thomas JB, Vivancos M, Giddings AM, Wiethe RW, Warner KR, Murza A, Besserer-Offroy É, Longpré JM, Runyon SP, Decker AM, Gilmour BP, Sarret P. Thomas JB, et al. ACS Chem Neurosci. 2016 Sep 21;7(9):1225-31. doi: 10.1021/acschemneuro.6b00097. Epub 2016 Jul 13. ACS Chem Neurosci. 2016. PMID: 27359371
332 results