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Akademický článek

Tolerance Mitigates Gall Effects When Susceptible Plants Fail to Elicit Induced Defense

Autor: Janete Ferreira Andrade, Eduardo Soares Calixto, Guilherme Ramos Demetrio, Henrique Venâncio, Marcos Vinicius Meiado, Denise Garcia de Santana, Pablo Cuevas-Reyes, Wanessa Rejane de Almeida, Jean Carlos Santos

Publikováno v: Plants, Vol 13, Iss 11, p 1472 (2024)

Variations in plant genotypes and phenotypes are expressed in ways that lead to the development of defensive abilities against herbivory. Induced defenses are mechanisms that affect herbivore insect preferences and performance. We evaluated the perfo

Externí odkaz: https://doaj.org/article/9bfbb2b9e56a4ecfaaabd2cac9d5d915

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Discovery of N-{4-[(3-Hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide Analogues as Selective Kappa Opioid Receptor Antagonists

Autor: Hernán A. Navarro, Chunyang Jin, Lawrence E. Brieaddy, Juan Pablo Cueva, Scott P. Runyon, F. Ivy Carroll, Chad M. Kormos, S. Wayne Mascarella, James B. Thomas, Brian P. Gilmour

Publikováno v: Journal of Medicinal Chemistry. 56:4551-4567

There is continuing interest in the discovery and development of new κ opioid receptor antagonists. We recently reported that N-substituted 3-methyl-4-(3-hydroxyphenyl)piperazines were a new class of opioid receptor antagonists. In this study, we re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e9743414a47193361c71935e9275711
https://doi.org/10.1021/jm400275h

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Analogues of doxanthrine reveal differences between the dopamine D1 receptor binding properties of chromanoisoquinolines and hexahydrobenzo[a]phenanthridines

Autor: Benjamin R. Chemel, Markus A. Lill, Val J. Watts, Jose I. Juncosa, David E. Nichols, Juan Pablo Cueva

Publikováno v: European Journal of Medicinal Chemistry. 48:97-107

Efforts to develop selective agonists for dopamine D(1)-like receptors led to the discovery of dihydrexidine and doxanthrine, two bioisosteric β-phenyldopamine-type full agonist ligands that display selectivity and potency at D(1)-like receptors. We

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::39023edbc047c5721db63a486028395c
https://doi.org/10.1016/j.ejmech.2011.11.039

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Probing the Steric Space at the Floor of the D1 Dopamine Receptor Orthosteric Binding Domain: 7α-, 7β-, 8α-, and 8β-Methyl Substituted Dihydrexidine Analogues

Autor: Markus A. Lill, David E. Nichols, Juan Pablo Cueva, Jose I. Juncosa, Val J. Watts, Alejandra Gallardo-Godoy, Pierre A. Vidi

Publikováno v: Journal of Medicinal Chemistry. 54:5508-5521

To probe the space at the floor of the orthosteric ligand binding site in the dopamine D(1) receptor, four methylated analogues of dihydrexidine (DHX) were synthesized with substitutions at the 7 and 8 positions. The 8α-axial, 8β-equatorial, and 7�

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acba383d690a9766c24f2f98d96045c5
https://doi.org/10.1021/jm200334c

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C-ring expanded analogs of doxanthrine: conformation plays a critical role

Autor: David E. Nichols, John D. McCorvy, Aubrie A. Harland, Juan Pablo Cueva, Alia H. Clark, Val J. Watts

Publikováno v: ARKIVOC, Vol 2010, Iss 4, Pp 125-138 (2011)

To assess the importance of conformation and placement of the β-substituent of agonist ligands targeted to the D1 dopamine receptor, (±)-trans-6,6a,7,8,13,13a-hexahydrobenzo[e]chromeno [3,4-b]azepine-2,3-diol 5 and (±)-trans-6,6a,7,8,9,13b-hexahyd

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d49cbf58a4601165c239a44ae84d6c2b
https://doi.org/10.3998/ark.5550190.0011.411

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1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists

Autor: Juan Pablo Cueva, Frank I. Carroll, Scott P. Runyon, James B. Thomas, Hernán A. Navarro, S. W. Mascarella

Publikováno v: ACS Medicinal Chemistry Letters. 1:365-369

This report describes the discovery that 1-substituted 4-(3-hydroxyphenyl)piperazines are pure opioid receptor antagonists. Compounds in this new series include N-phenylpropyl (3S)-3-methyl-4-(3-hydroxyphenyl)piperazine and (3R)-3-methyl-4-(3-hydroxy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee2d93f88e1b6bb2c6ee58f87289878b
https://doi.org/10.1021/ml100126b

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Synthesis and In Vitro Opioid Receptor Functional Antagonism of Methyl-Substituted 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)

Autor: Juan Pablo Cueva, F. Ivy Carroll, Hernán A. Navarro, Tingwei Bill Cai, James B. Thomas, S. Wayne Mascarella

Publikováno v: Journal of Medicinal Chemistry. 52:7463-7472

In previous structure−activity relationship (SAR) studies, (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, 3) was identified as the first

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5ae6d7baca3a7ace1dc732c0381e16bd
https://doi.org/10.1021/jm900756t

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A Novel and Efficient Synthesis of Dihydrexidine

Autor: David E. Nichols, Juan Pablo Cueva

Publikováno v: Synthesis. 2009:715-720

An efficient synthesis of the dopamine D 1 selective full agonist dihydrexidine has been achieved in high yields and requiring no chromatographic separations via a facilitated intramolecular Henry cyclization of a (nitropropyl)benzophenone and subseq

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e931b42e2061f3f46b66820f231ada4c
https://doi.org/10.1055/s-0028-1083359

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C7β-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors

Autor: Juan Pablo Cueva, Mary J. Clark, John W. Lewis, Vinod Kumar, Stephen M. Husbands, Christopher Roche, John R. Traynor, Todd M. Hillhouse, Mehrnoosh Ostovar

Publikováno v: Journal of Medicinal Chemistry
Cueva, J P, Roche, C, Ostovar, M, Kumar, V, Clark, M J, Hillhouse, T M, Lewis, J W, Traynor, J R & Husbands, S M 2015, ' C7β-Methyl Analogues of the Orvinols : The Discovery of Kappa Opioid Antagonists with Nociceptin/Orphanin FQ Peptide (NOP) Receptor Partial Agonism and Low, or Zero, Efficacy at Mu Opioid Receptors ', Journal of Medicinal Chemistry, vol. 58, no. 10, pp. 4242-4249 . https://doi.org/10.1021/acs.jmedchem.5b00130

Buprenorphine is a successful analgesic and treatment for opioid abuse, with both activities relying on its partial agonist activity at mu opioid receptors. However, there is substantial interest in its activities at the kappa opioid and nociceptin/o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9cf40402f9f7b21bf0af69c63f64947
https://pubmed.ncbi.nlm.nih.gov/25898137

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