Zobrazeno 1 - 10
of 328
pro vyhledávání: '"Arthur E, Jacobson"'
Autor:
Hudson G. Roth, Madhurima Das, Agnieszka Sulima, Dan Luo, Sophia Kaska, Thomas E. Prisinzano, Andrew T. Kerr, Arthur E. Jacobson, Kenner C. Rice
Publikováno v:
Molecules, Vol 29, Iss 9, p 1926 (2024)
The synthesis of stereochemically pure oximes, amines, saturated and unsaturated cyanomethyl compounds, and methylaminomethyl compounds at the C9 position in 3-hydroxy-N-phenethyl-5-phenylmorphans provided μ-opioid receptor (MOR) agonists with varie
Externí odkaz:
https://doaj.org/article/ffafaa3d32ea40d5bd3043c657d40a47
Autor:
Edna J. Santos, Nima Nassehi, Eric W. Bow, Dana R. Chambers, Eugene S. Gutman, Arthur E. Jacobson, Joshua A. Lutz, Samuel A. Marsh, Kenner C. Rice, Agnieszka Sulima, Dana E. Selley, S. Stevens Negus
Publikováno v:
Pharmacology Research & Perspectives, Vol 11, Iss 4, Pp n/a-n/a (2023)
Abstract Low‐efficacy mu‐opioid receptor (MOR) agonists represent promising therapeutics, but existing compounds (e.g., buprenorphine, nalbuphine) span a limited range of low MOR efficacies and have poor MOR selectivity. Accordingly, new and sele
Externí odkaz:
https://doaj.org/article/3416c03aeec64d3f8a90e94380e1ee04
Autor:
Madhurima Das, George W. Ward, Agnieszka Sulima, Dan Luo, Thomas Edward Prisinzano, Gregory H. Imler, Andrew T. Kerr, Arthur E. Jacobson, Kenner C. Rice
Publikováno v:
Molecules, Vol 28, Iss 23, p 7709 (2023)
(−)-5,9-Dimethyl-6,7-benzomorphan (normetazocine) derivatives with a para-OH or ortho-F substituent in the aromatic ring of the N-phenethyl moiety were synthesized and found to have subnanomolar potency at MOR, and both were fully efficacious in vi
Externí odkaz:
https://doaj.org/article/9bbb663c8248404c9ee45202cb61671a
Autor:
Dana R. Chambers, Agnieszka Sulima, Dan Luo, Thomas E. Prisinzano, Arthur E. Jacobson, Kenner C. Rice
Publikováno v:
Molecules, Vol 28, Iss 14, p 5411 (2023)
The 5-(3-hydroxy)phenylmorphan structural class of compounds are unlike the classical morphinans, 4,5-epoxymorphinans, and 6,7-benzomorphans, in that they have an equatorially oriented aromatic ring rather than the axial orientation of that ring foun
Externí odkaz:
https://doaj.org/article/1173e73197ae44f09a580ac3675e041b
Autor:
Joshua A. Lutz, Agnieszka Sulima, Eugene S. Gutman, Eric W. Bow, Dan Luo, Sophia Kaska, Thomas E. Prisinzano, Carol A. Paronis, Jack Bergman, Gregory H. Imler, Andrew T. Kerr, Arthur E. Jacobson, Kenner C. Rice
Publikováno v:
Molecules, Vol 28, Iss 12, p 4795 (2023)
All possible diastereomeric C9-hydroxymethyl-, hydroxyethyl-, and hydroxypropyl-substituted 5-phenylmorphans were synthesized to explore the three-dimensional space around the C9 substituent in our search for potent MOR partial agonists. These compou
Externí odkaz:
https://doaj.org/article/d4aecd3b74884423a75e5b6fc1efb0c0
Publikováno v:
Results in Chemistry, Vol 4, Iss , Pp 100390- (2022)
Two modifications of previous procedures enabled the high-yield scalable synthesis of the pharmacologically important enantiomers of a C9-keto-5-phenylmorphan ((1R,5R)- and (1S,5S)-5-(3-methoxyphenyl)-2-methyl-2-azabicyclo[3.3.1]nonan-9-one). The use
Externí odkaz:
https://doaj.org/article/73dd035c57744f8aaacb06c43321a873
Autor:
Fuying Li, Theresa A. Kopajtic, Jonathan L. Katz, Dan Luo, Thomas E. Prisinzano, Gregory H. Imler, Jeffrey R. Deschamps, Arthur E. Jacobson, Kenner C. Rice
Publikováno v:
Molecules, Vol 27, Iss 24, p 8808 (2022)
The design of enantiopure stereoisomers of N-2-phenylcyclopropylmethyl-substituted ortho-c oxide-bridged phenylmorphans, the E and Z isomers of an N-cinnamyl moiety, and N-propyl enantiomers were based on combining the most potent oxide-bridged pheny
Externí odkaz:
https://doaj.org/article/527163ca03564816a00891ccd82a9e1f
Autor:
Dana R. Chambers, Agnieszka Sulima, Dan Luo, Thomas E. Prisinzano, Alexander Goldberg, Bing Xie, Lei Shi, Carol A. Paronis, Jack Bergman, Nima Nassehi, Dana E. Selley, Gregory H. Imler, Arthur E. Jacobson, Kenner C. Rice
Publikováno v:
Molecules, Vol 27, Iss 19, p 6455 (2022)
Four sets of diastereomeric C9-alkenyl 5-phenylmorphans, varying in the length of the C9-alkenyl chain, were designed to examine the effect of these spatially distinct ligands on opioid receptors. Functional activity was obtained by forskolin-induced
Externí odkaz:
https://doaj.org/article/d9c38bdcc69f493eb1644c1632588662
Autor:
Bhupal Ban, Rodell C. Barrientos, Therese Oertel, Essie Komla, Connor Whalen, Megan Sopko, Yingjian You, Partha Banerjee, Agnieszka Sulima, Arthur E. Jacobson, Kenner C. Rice, Gary R. Matyas, Vidadi Yusibov
Publikováno v:
mAbs, Vol 13, Iss 1 (2021)
The prevalence and societal impact of opioid use disorder (OUD) is an acknowledged public health crisis that is further aggravated by the current pandemic. One of the devastating consequences of OUD is opioid overdose deaths. While multiple medicatio
Externí odkaz:
https://doaj.org/article/a57dc3421a724889a100c3b2663a617c
Autor:
Agnieszka Sulima, Fuying Li, Jeffrey Brian Morgan, Phong Truong, Joshua F. G. Antoline, Therese Oertel, Rodell C. Barrientos, Oscar B. Torres, Zoltan Beck, Gregory H. Imler, Jeffrey R. Deschamps, Gary R. Matyas, Arthur E. Jacobson, Kenner C. Rice
Publikováno v:
Molecules, Vol 27, Iss 5, p 1553 (2022)
In our continuing effort to develop effective anti-heroin vaccines as potential medications for the treatment of opioid use disorder, herein we present the design and synthesis of the haptens: 1-AmidoMorHap (1), 1-AmidoMorHap epimer (2), 1 Amido-Dihy
Externí odkaz:
https://doaj.org/article/7dcc4f534c6c4cc6b767b5b5ab286a1c