Zobrazeno 1 - 10
of 69
pro vyhledávání: '"Marián Castro"'
Autor:
Filipe Areias, Carla Correia, Ashly Rocha, Sofia Teixeira, Marián Castro, Jose Brea, Huabin Hu, Jens Carlsson, Maria I. Loza, M. Fernanda Proença, M. Alice Carvalho
Publikováno v:
Molecules, Vol 29, Iss 11, p 2543 (2024)
A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A1, A2A, A2B, and A3 adenosine receptor subtypes. Eleven purines showed potent antagonism at A1, A3, dual A1/A2A, A1/
Externí odkaz:
https://doaj.org/article/7cbea8944ba641e096dee5b96a2e909e
Autor:
Piotr Stępnicki, Olga Wronikowska-Denysiuk, Agata Zięba, Katarzyna M. Targowska-Duda, Agata Bartyzel, Martyna Z. Wróbel, Tomasz M. Wróbel, Klaudia Szałaj, Andrzej Chodkowski, Karolina Mirecka, Barbara Budzyńska, Emilia Fornal, Jadwiga Turło, Marián Castro, Agnieszka A. Kaczor
Publikováno v:
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1 (2023)
Schizophrenia is a chronic mental disorder that is not satisfactorily treated with available antipsychotics. The presented study focuses on the search for new antipsychotics by optimising the compound D2AAK3, a multi-target ligand of G-protein-couple
Externí odkaz:
https://doaj.org/article/7d0e4b8d609e40c3b4670a0604436c47
Autor:
Piotr Stępnicki, Sylwia Wośko, Agata Bartyzel, Agata Zięba, Damian Bartuzi, Klaudia Szałaj, Tomasz M. Wróbel, Emilia Fornal, Jens Carlsson, Ewa Kędzierska, Ewa Poleszak, Marián Castro, Agnieszka A. Kaczor
Publikováno v:
Molecules, Vol 28, Iss 10, p 4211 (2023)
The dopamine D2 receptor, which belongs to the family of G protein-coupled receptors (GPCR), is an important and well-validated drug target in the field of medicinal chemistry due to its wide distribution, particularly in the central nervous system,
Externí odkaz:
https://doaj.org/article/9722a60b29344f989fa26a12ffad5099
Autor:
Margherita Mastromarino, Mauro Niso, Carmen Abate, Ewgenij Proschak, Mariam Dubiel, Holger Stark, Marián Castro, Enza Lacivita, Marcello Leopoldo
Publikováno v:
Molecules, Vol 27, Iss 4, p 1297 (2022)
Long-chain arylpiperazine scaffold is a versatile template to design central nervous system (CNS) drugs that target serotonin and dopamine receptors. Here we describe the synthesis and biological evaluation of ten new arylpiperazine derivatives desig
Externí odkaz:
https://doaj.org/article/e03fb4ce8fd04f57bd7789c1a958706f
Autor:
Agnieszka A. Kaczor, Katarzyna M. Targowska-Duda, Andrea G. Silva, Magda Kondej, Grażyna Biała, Marián Castro
Publikováno v:
Biomolecules, Vol 10, Iss 2, p 349 (2020)
N-(2-hydroxyphenyl)-1-[3-(2-oxo-2,3-dihydro-1H-benzimidazol -1-yl)propyl]piperidine-4-carboxamide (D2AAK4) is a multitarget ligand of aminergic G protein-coupled receptors (GPCRs) identified in structure-based virtual screening. Here we present detai
Externí odkaz:
https://doaj.org/article/72233e18ddee4a749cde3915681b2ca5
Autor:
Ana Bettencourt, Marián Castro, João Silva, Francisco Fernandes, Olga Coutinho, M. João Sousa, M. Fernanda Proença, Filipe Areias
Publikováno v:
Molecules, Vol 23, Iss 10, p 2530 (2018)
A selection of 1-amino-2-arylidenamine-1,2-(dicyano)ethenes 3 was synthesized and cyclized to 2-aryl-4,5-dicyano-1H-imidazoles 4 upon reflux in ethyl acetate/acetonitrile, in the presence of manganese dioxide. These compounds were tested for their an
Externí odkaz:
https://doaj.org/article/d0542d8b37f5466c8bad75f0c23d48b7
Autor:
Magda Kondej, Agata Bartyzel, Monika Pitucha, Tomasz M. Wróbel, Andrea G. Silva, Dariusz Matosiuk, Marián Castro, Agnieszka A. Kaczor
Publikováno v:
Molecules, Vol 23, Iss 9, p 2249 (2018)
Compound D2AAK1_3 was designed as a modification of the lead structure D2AAK1 (an in vivo active multi-target compound with nanomolar affinity to a number of aminergic GPCRs) and synthesized in the reaction of 5-ethoxyindole and 1-benzyl-4-piperidone
Externí odkaz:
https://doaj.org/article/c585186ac5fe417f842edcb74098a199
Autor:
Oliwia Koszła, Przemysław Sołek, Ewa Kędzierska, Piotr Listos, Marián Castro, Agnieszka A. Kaczor
Publikováno v:
Neurochemical Research. 47:1778-1789
The susceptibility of neurons to free radical toxicity partially underlies the pathomechanism of neurodegenerative diseases. On the other hand, excitotoxicity also contributes to neurodegeneration. Our previous studies demonstrated the unique propert
Autor:
Justyna Żuk, Damian Bartuzi, Andrea G. Silva, Monika Pitucha, Oliwia Koszła, Tomasz M. Wróbel, Dariusz Matosiuk, Marián Castro, Agnieszka A. Kaczor
Publikováno v:
Pharmacological Reports. 74:406-424
Background Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays one of the hot topics in drug discovery. In particular, allosteric modulators of D2 receptor have been proposed as potential modern therapeutics to treat schizophreni
Autor:
Magda Kondej, Tomasz M. Wróbel, Katarzyna M. Targowska‐Duda, Antón Leandro Martínez, Oliwia Koszła, Piotr Stępnicki, Agata Zięba, Alba Paz, Olga Wronikowska‐Denysiuk, Maria I. Loza, Marián Castro, Agnieszka A. Kaczor
Publikováno v:
ChemMedChem. 17(15)
Schizophrenia is a complex disease which is best treated with multitarget drugs, such as atypical antipsychotics. Previously, using structure-based virtual screening, we found a virtual hit, D2AAK1, with nanomolar affinity for dopamine and serotonin