Full Text Journal Articles by
Author Ignacio Moraleda

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Synthesis of Hantzsch Adducts as Cholinesterases and Calcium Flux inhibitors, Antioxidants and Neuroprotectives.

Irene Pachón Angona, Helene Martin, Solene Daniel, Ignacio Moraleda, Alexandre Bonet, Artur Wnorowski, Maciej Maj, Krzysztof Jozwiak, Isabel Iriepa, Bernard Refouvelet, José Marco-Contelles, Lhassane Ismaili,

We report herein the design, synthesis, biological evaluation, and molecular modelling of new inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), able to block Ca<sup>+2</sup> channels also showing antioxidant and neuroprotective activities. The new MTDL, dialkyl 2,6-dimethyl-4-(4-((5-aminoalkyl)oxy)phenyl)-1,4-dihydropyridine-3,5-dicarboxylate <b>3a-p</b>, have been obtained via Hantzsch reaction from appropriate and commercially available precursors. Pertinent ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2020, 21(20):]

Cited: 1 time

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New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition.

Rim Malek, Raquel L Arribas, Alejandra Palomino-Antolin, Perle Totoson, Celine Demougeot, Tereza Kobrlova, Ondrej Soukup, Isabel Iriepa, Ignacio Moraleda, Daniel Diez-Iriepa, Justyna Godyń, Dawid Panek, Barbara Malawska, Monika Głuch-Lutwin, Barbara Mordyl, Agata Siwek, Fakher Chabchoub, José Marco-Contelles, Katarzyna Kiec-Kononowicz, Javier Egea, Cristóbal de Los Ríos, Lhassane Ismaili,

New tritarget small molecules combining Ca2+ channels blockade, cholinesterase, and H3 receptor inhibition were obtained by multicomponent synthesis. Compound 3p has been identified as a very promising lead, showing good Ca2+ channels blockade activity (IC50 = 21 ± 1 μM), potent affinity against hH3R (Ki = 565 ± 62 nM), ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2019, 62(24):11416-11422]

Cited: 6 times

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Donepezil + chromone + melatonin hybrids as promising agents for Alzheimer's disease therapy.

Irene Pachón-Angona, Bernard Refouvelet, Rudolf Andrýs, Helène Martin, Vincent Luzet, Isabel Iriepa, Ignacio Moraleda, Daniel Diez-Iriepa, María-Jesús Oset-Gasque, José Marco-Contelles, Kamil Musilek, Lhassane Ismaili,

We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC<sub>50</sub> = 11.90 ± 0.05 nM), moderate hAChE (IC<sub>50</sub> = 1.73 ± 0.34 μM), hMAO A (IC<sub>50</sub> = 2.78 ± 0.12 μM), and MAO B (IC<sub>50</sub> = 21.29 ± 3.85 μM) inhibition, while keeping ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2019, 34(1):479-489]

Cited: 9 times

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Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer's disease therapy.

Youssef Dgachi, Hélène Martin, Rim Malek, Daniel Jun, Jana Janockova, Vendula Sepsova, Ondrej Soukup, Isabel Iriepa, Ignacio Moraleda, Emna Maalej, M Carmo Carreiras, Bernard Refouvelet, Fakher Chabchoub, José Marco-Contelles, Lhassane Ismaili,

In view of the multifactorial nature of Alzheimer's disease (AD), multitarget small molecules (MTSM) represent the most potent and attractive therapeutic strategy to design new drugs for Alzheimer's disease therapy. The new MTSM KojoTacrines (KTs) were designed and synthesized by juxtaposition of selected pharmacophoric motifs from kojic acid and tacrine. ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2019, 34(1):163-170]

Cited: 2 times

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Multi-target 1,4-dihydropyridines showing calcium channel blockade and antioxidant capacity for Alzheimer's disease therapy.

Rim Malek, Maciej Maj, Artur Wnorowski, Krzysztof Jóźwiak, Helene Martin, Isabel Iriepa, Ignacio Moraleda, Fakher Chabchoub, José Marco-Contelles, Lhassane Ismaili,

In this work we describe the synthesis, Ca<sup>+2</sup> channel blockade capacity and antioxidant power of N<sup>3</sup>,N<sup>5</sup>-bis(2-(5-methoxy-1H-indol-3-yl)ethyl)-2,6-dimethyl-4-aryl-1,4-dihydropyridine-3,5-dicarboxamides 1-9, a number of multi-target small 1,4-dihydropyridines (DHP), designed by juxtaposition of melatonin and nimodipine. As a result, we have identified antioxidant DHP 7 (Ca<sup>2+</sup> channel blockade: 55%, and 8.78 Trolox/Equivalents), the most balanced ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2019, 91:103205]

Cited: 5 times

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QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer's Disease Therapy.

Eva Ramos, Alejandra Palomino-Antolín, Manuela Bartolini, Isabel Iriepa, Ignacio Moraleda, Daniel Diez-Iriepa, Abdelouahid Samadi, Carol V Cortina, Mourad Chioua, Javier Egea, Alejandro Romero, José Marco-Contelles,

We report the synthesis and relevant pharmacological properties of the quinoxalinetacrine (QT) hybrid <b>QT78</b> in a project targeted to identify new non-hepatotoxic tacrine derivatives for Alzheimer's disease therapy. We have found that <b>QT78</b> is less toxic than tacrine at high concentrations (from 100 μM to 1 mM), less potent than ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2019, 24(8):]

Cited: 3 times

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Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.

Serena Montanari, Ali Mokhtar Mahmoud, Letizia Pruccoli, Alessandro Rabbito, Marina Naldi, Sabrina Petralla, Ignacio Moraleda, Manuela Bartolini, Barbara Monti, Isabel Iriepa, Federica Belluti, Silvia Gobbi, Vincenzo Di Marzo, Alessandra Bisi, Andrea Tarozzi, Alessia Ligresti, Angela Rampa,

To address the multifactorial nature of Alzheimer's Disease (AD), a multi-target-directed ligand approach was herein developed. As a follow-up of our previous studies, a small library of newly designed 2-arylbenzofuran derivatives was evaluated towards cholinesterases and cannabinoid receptors. The two most promising compounds, 8 and 10, were then assessed for ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 178:243-258]

Cited: 3 times

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Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.

Ehab D AlFadly, Perihan A Elzahhar, Anna Tramarin, Salwa Elkazaz, Hossam Shaltout, Marwa M Abu-Serie, Jana Janockova, Ondrej Soukup, Doaa A Ghareeb, Ahmed F El-Yazbi, Rim W Rafeh, Nour-Mounira Z Bakkar, Firas Kobeissy, Isabel Iriepa, Ignacio Moraleda, Manal N S Saudi, Manuela Bartolini, Ahmed S F Belal,

Neuroinflammation and cholinergic deficit are key detrimental processes involved in Alzheimer's disease. Hence, in the search for novel and effective treatment strategies, the multi-target-directed ligand paradigm was applied to the rational design of two series of new hybrids endowed with anti-inflammatory and anticholinesterase activity via triple targeting properties, namely able ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 167:161-186]

Cited: 7 times

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Synthesis and Biological Evaluation of Novel Chromone+Donepezil Hybrids for Alzheimer's Disease Therapy.

Rim Malek, Bernard Refouvelet, Mohamed Benchekroun, Isabel Iriepa, Ignacio Moraleda, Rudolf Andrys, Kamil Musilek, José Marco-Contelles, Lhassane Ismaili,

<h4>Background</h4>Many factors are involved in Alzheimer's Disease (AD) such as amyloid plaques, neurofibrillary tangles, cholinergic deficit and oxidative stress. To counter the complexity of the disease the new approach for drug development is to create a single molecule able to act simultaneously on different targets.<h4>Objective</h4>We conceived eight drug likeliness compounds ... Read more >>

Curr Alzheimer Res (Current Alzheimer research)
[2019, 16(9):815-820]

Cited: 1 time

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Exploiting the Chalcone Scaffold to Develop Multifunctional Agents for Alzheimer's Disease.

Angela Rampa, Manuela Bartolini, Letizia Pruccoli, Marina Naldi, Isabel Iriepa, Ignacio Moraleda, Federica Belluti, Silvia Gobbi, Andrea Tarozzi, Alessandra Bisi,

Alzheimer's disease still represents an untreated multifaceted pathology, and drugs able to stop or reverse its progression are urgently needed. In this paper, a series of naturally inspired chalcone-based derivatives were designed as structural simplification of our previously reported benzofuran lead compound, aiming at targeting both acetyl (AChE)- and butyryl ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2018, 23(8):]

Cited: 6 times

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Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.

Óscar M Bautista-Aguilera, Josiane Budni, Francielle Mina, Eduarda Behenck Medeiros, Winnie Deuther-Conrad, José M Entrena, Ignacio Moraleda, Isabel Iriepa, Francisco López-Muñoz, José Marco-Contelles,

Contilisant, a permeable, antioxidant, and neuroprotectant agent, showing high nM affinity at H3R and excellent inhibition of the monoamine oxidases and cholinesterases, is an affine and selective S1R agonist in the nanomolar range, based on the binding affinity and functional experiment, a result confirmed by molecular modeling. In addition, contilisant ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2018, 61(15):6937-6943]

Cited: 7 times

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Tacripyrimidines, the first tacrine-dihydropyrimidine hybrids, as multi-target-directed ligands for Alzheimer's disease.

Mourad Chioua, Eleonora Buzzi, Ignacio Moraleda, Isabel Iriepa, Maciej Maj, Artur Wnorowski, Catia Giovannini, Anna Tramarin, Federica Portali, Lhassane Ismaili, Pilar López-Alvarado, Maria Laura Bolognesi, Krzysztof Jóźwiak, J Carlos Menéndez, José Marco-Contelles, Manuela Bartolini,

Notwithstanding the combination of cholinesterase (ChE) inhibition and calcium channel blockade within a multitarget therapeutic approach is envisaged as potentially beneficial to confront Alzheimer's disease (AD), this strategy has been scarcely investigated. To explore this promising line, a series of 5-amino-4-aryl-3,4,6,7,8,9-hexahydropyrimido [4,5-b]quinoline-2(1H)-thiones (tacripyrimidines) (4a-l) were designed by juxtaposition of tacrine, ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2018, 155:839-846]

Cited: 9 times

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Poly(amidoamine) dendrimers grafted on electrospun poly(acrylic acid)/poly(vinyl alcohol) membranes for host-guest encapsulation of antioxidant thymol.

Georgiana Amariei, Karina Boltes, Pedro Letón, Isabel Iriepa, Ignacio Moraleda, Roberto Rosal,

Amino-terminated fifth generation poly(amidoamine) (PAMAM G5-NH2) dendrimers were grafted onto the surface of poly(acrylic acid)/poly(vinyl alcohol) (PAA/PVA) electrospun fibres with the purpose of creating a host-guest architecture for the controlled delivery of a natural antioxidant, thymol. The nanofibers were stabilized by esterification crosslinking to produce a water insoluble non-woven membrane. ... Read more >>

J Mater Chem B (Journal of materials chemistry. B)
[2017, 5(33):6776-6785]

Cited: 2 times

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Dendrimer-functionalized electrospun nanofibres as dual-action water treatment membranes.

Georgiana Amariei, Javier Santiago-Morales, Karina Boltes, Pedro Letón, Isabel Iriepa, Ignacio Moraleda, Amadeo R Fernández-Alba, Roberto Rosal,

This work reports the preparation of composite electrospun membranes combining antimicrobial action with the capacity of retaining low-molecular weight non-polar pollutants. The membranes were electrospun blends of polyvinyl alcohol (PVA) and poly(acrylic acid) (PAA) stabilized using heat curing. The membranes were functionalized by grafting amino-terminated poly(amidoamine) (PAMAM) G3 dendrimers. The ... Read more >>

Sci Total Environ (The Science of the total environment)
[2017, 601-602:732-740]

Cited: 2 times

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Multitarget-Directed Ligands Combining Cholinesterase and Monoamine Oxidase Inhibition with Histamine H3 R Antagonism for Neurodegenerative Diseases.

Óscar M Bautista-Aguilera, Stefanie Hagenow, Alejandra Palomino-Antolin, Víctor Farré-Alins, Lhassane Ismaili, Pierre-Louis Joffrin, María L Jimeno, Ondřej Soukup, Jana Janočková, Lena Kalinowsky, Ewgenij Proschak, Isabel Iriepa, Ignacio Moraleda, Johannes S Schwed, Alejandro Romero Martínez, Francisco López-Muñoz, Mourad Chioua, Javier Egea, Rona R Ramsay, José Marco-Contelles, Holger Stark,

The therapy of complex neurodegenerative diseases requires the development of multitarget-directed drugs (MTDs). Novel indole derivatives with inhibitory activity towards acetyl/butyrylcholinesterases and monoamine oxidases A/B as well as the histamine H<sub>3</sub> receptor (H3R) were obtained by optimization of the neuroprotectant ASS234 by incorporating generally accepted H3R pharmacophore motifs. These small-molecule ... Read more >>

Angew Chem Int Ed Engl (Angewandte Chemie (International ed. in English))
[2017, 56(41):12765-12769]

Cited: 17 times

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5-Methyl-N-(8-(5,6,7,8-tetrahydroacridin-9-ylamino)octyl)-5H-indolo[2,3-b]quinolin-11-amine: a highly potent human cholinesterase inhibitor.

Li Wang, Ignacio Moraleda, Isabel Iriepa, Alejandro Romero, Francisco López-Muñoz, Mourad Chioua, Tsutomu Inokuchi, Manuela Bartolini, José Marco-Contelles,

The synthesis, cholinesterase inhibition, molecular modelling and ADME properties of novel tacrine-neocryptolepine heterodimers are described. Compound <b>3</b> [5-methyl-<i>N</i>-(8-(5,6,7,8-tetrahydroacridin-9-ylamino)octyl)-5<i>H</i>-indolo[2,3-<i>b</i>]quinolin-11-amine], showing a moderate inhibition of the Aβ<sub>1-42</sub> self-aggregation (26.5% at a 1 : 5 ratio with Aβ<sub>1-42</sub>), and a calculated log BB value (0.27) indicating excellent potential BBB penetration, is a highly potent human cholinesterase ... Read more >>

Medchemcomm (MedChemComm)
[2017, 8(6):1307-1317]

Cited: 2 times

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Synthesis and biological assessment of racemic benzochromenopyrimidinetriones as promising agents for Alzheimer's disease therapy.

Youssef Dgachi, Helène Martin, Alexandre Bonet, Mourad Chioua, Isabel Iriepa, Ignacio Moraleda, Fakher Chabchoub, José Marco-Contelles, Lhassane Ismaili,

<h4>Aim</h4>Due to the complex nature of Alzheimer's disease, there is a renewed search for multitarget directed drugs.<h4>Results</h4>This paper describes the synthesis and in vitro biological evaluation of six racemic 13-aryl-2,3,4,13-tetrahydro-1H,12H-benzo[6,7]chromeno[2,3-d]pyrido[1,2-a]pyrimidine-7,12,14-triones (1a-6a), and six racemic 15-aryl-8,9,10,11,12,15-hexahydro-14H-benzo[6',7']chromeno[2',3:4,5] pyr-imido [1,2-a]azepine-5,14,16-triones (1b-6b), showing antioxidant and cholinesterase inhibitory capacity. Among these compounds, 13-phenyl-2,3,4,13-tetrahydro-1H,12H-benzo[6,7]chromeno[2,3-d]pyrido[1,2-a]pyrimidine-7,12,14-trione (1a) is ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2017, 9(8):715-721]

Cited: 1 time

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Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy.

Youssef Dgachi, Olga Sokolov, Vincent Luzet, Justyna Godyń, Dawid Panek, Alexandre Bonet, Hélène Martin, Isabel Iriepa, Ignacio Moraleda, Cristina García-Iriepa, Jana Janockova, Lysiane Richert, Ondrej Soukup, Barbara Malawska, Fakher Chabchoub, José Marco-Contelles, Lhassane Ismaili,

Herein we report an efficient two step synthesis and biological assessment of 12 racemic tetrahydropyranodiquinolin-8-amines derivatives as antioxidant, cholinesterase inhibitors and non-hepatotoxic agents. Based on the results of the primary screening, we identified 7-(3-methoxyphenyl)-9,10,11,12-tetrahydro-7H-pyrano[2,3-b:5,6-h']diquinolin-8-amine (2h) as a particularly interesting non-hepatotoxic compound that shows moderate antioxidant activity (1.83 equiv Trolox in ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2017, 126:576-589]

Cited: 7 times

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Potent anticholinesterasic and neuroprotective pyranotacrines as inhibitors of beta-amyloid aggregation, oxidative stress and tau-phosphorylation for Alzheimer's disease.

Nuria García-Font, Hasna Hayour, Ali Belfaitah, Jorge Pedraz, Ignacio Moraleda, Isabel Iriepa, Abdelmalek Bouraiou, Mourad Chioua, José Marco-Contelles, María Jesús Oset-Gasque,

Herein we describe the synthesis and in vitro biological evaluation of thirteen new, racemic, diversely functionalized 2-chloroquinolin-3-yl substituted PyranoTacrines (PTs) as multipotent tacrine analogues for Alzheimer's disease (AD) therapy. Among these compounds, 1-(5-amino-4-(2-chloro-7-methoxyquinolin-3-yl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrano [2,3-b]quinolin-3-yl)éthanone (9) and ethyl 5-amino-4-(2-chloroquinolin-3-yl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrano[2,3-b]quinoline-3-carboxylate (4) were found to be non-neurotoxic agents in human neuroblastoma SHSY5Y cells. Compounds ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2016, 118:178-192]

Cited: 11 times

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Imidazopyranotacrines as Non-Hepatotoxic, Selective Acetylcholinesterase Inhibitors, and Antioxidant Agents for Alzheimer's Disease Therapy.

Houssem Boulebd, Lhassane Ismaili, Manuela Bartolini, Abdelmalek Bouraiou, Vincenza Andrisano, Helene Martin, Alexandre Bonet, Ignacio Moraleda, Isabel Iriepa, Mourad Chioua, Ali Belfaitah, José Marco-Contelles,

Herein we describe the synthesis and in vitro biological evaluation of thirteen new, racemic, diversely functionalized imidazo pyranotacrines as non-hepatotoxic, multipotent tacrine analogues. Among these compounds, 1-(5-amino-2-methyl-4-(1-methyl-1H-imidazol-2-yl)-6,7,8,9-tetrahydro-4H-pyrano[2,3-b]quinolin-3-yl)ethan-1-one (4) is non-hepatotoxic (cell viability assay on HepG2 cells), a selective but moderately potent EeAChE inhibitor (IC50 = 38.7 ± 1.7 μM), and ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2016, 21(4):400]

Cited: 2 times

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Harmaline and hispidin from Peganum harmala and Inonotus hispidus with binding affinity to Candida rugosa lipase: In silico and in vitro studies.

Khedidja Benarous, Isabelle Bombarda, Isabel Iriepa, Ignacio Moraleda, Herbette Gaetan, Abderrahmane Linani, Djillali Tahri, Mohamed Sebaa, Mohamed Yousfi,

The inhibitory effect of phenolic compounds and alkaloids of Inonotus hispidus and Peganum harmala on Candida rugosa lipase was investigated, also, their antioxidant activities using DPPH, ABTS and phosphomolybdenum were studied in this paper. The phenolic extracts have shown a stronger antiradical activity than the alkaloids extracts. The enzymatic inhibition ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2015, 62:1-7]

Cited: 4 times

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Pyranopyrazolotacrines as nonneurotoxic, Aβ-anti-aggregating and neuroprotective agents for Alzheimer's disease.

Mourad Chioua, Javier Pérez-Peña, Nuria García-Font, Ignacio Moraleda, Isabel Iriepa, Elena Soriano, José Marco-Contelles, María Jesús Oset-Gasque,

<h4>Aim</h4>Due to the complex nature of Alzheimer's disease, there is a renewed search for multipotent, nonhepatotoxic tacrines.<h4>Results</h4>This paper describes the synthesis and in vitro biological evaluation of eight new racemic 3-methyl-4-aryl-2,4,6,7,8,9-hexahydropyrazolo[4',3':5,6]pyrano[2,3-b]quinolin-5-amines (pyranopyrazolotacrines, PPT) as nonhepatotoxic multipotent tacrine analogs. Among these compounds, PPT4 is the less hepatotoxic in the cell viability ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2015, 7(7):845-855]

Cited: 6 times

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Multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease: design, synthesis, biochemical evaluation, ADMET, molecular modeling, and QSAR analysis of novel donepezil-pyridyl hybrids.

Oscar M Bautista-Aguilera, Gerard Esteban, Mourad Chioua, Katarina Nikolic, Danica Agbaba, Ignacio Moraleda, Isabel Iriepa, Elena Soriano, Abdelouahid Samadi, Mercedes Unzeta, José Marco-Contelles,

The design, synthesis, and biochemical evaluation of donepezil-pyridyl hybrids (DPHs) as multipotent cholinesterase (ChE) and monoamine oxidase (MAO) inhibitors for the potential treatment of Alzheimer's disease (AD) is reported. The 3D-quantitative structure-activity relationship study was used to define 3D-pharmacophores for inhibition of MAO A/B, acetylcholinesterase (AChE), and butyrylcholinesterase (BuChE) enzymes ... Read more >>

Drug Des Devel Ther (Drug design, development and therapy)
[2014, 8:1893-1910]

Cited: 19 times

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Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease.

Li Wang, Gerard Esteban, Masaki Ojima, Oscar M Bautista-Aguilera, Tsutomu Inokuchi, Ignacio Moraleda, Isabel Iriepa, Abdelouahid Samadi, Moussa B H Youdim, Alejandro Romero, Elena Soriano, Raquel Herrero, Ana Patricia Fernández Fernández, Ricardo-Martínez-Murillo, José Marco-Contelles, Mercedes Unzeta,

The synthesis, biochemical evaluation, ADMET, toxicity and molecular modeling of novel multi-target-directed Donepezil + Propargylamine + 8-Hydroxyquinoline (DPH) hybrids 1-7 for the potential prevention and treatment of Alzheimer's disease is described. The most interesting derivative was racemic α-aminotrile4-(1-benzylpiperidin-4-yl)-2-(((8-hydroxyquinolin-5-yl)methyl)(prop-2-yn-1-yl)amino) butanenitrile (DPH6) [MAO A (IC50 = 6.2 ± 0.7 μM; MAO B ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2014, 80:543-561]

Cited: 40 times

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Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.

Oscar M Bautista-Aguilera, Gerard Esteban, Irene Bolea, Katarina Nikolic, Danica Agbaba, Ignacio Moraleda, Isabel Iriepa, Abdelouahid Samadi, Elena Soriano, Mercedes Unzeta, José Marco-Contelles,

The design, synthesis, and pharmacological evaluation of donepezil-indolyl based amines 7-10, amides 12-16, and carboxylic acid derivatives 5 and 11, as multipotent ASS234 analogs, able to inhibit simultaneously cholinesterase (ChE) and monoamine oxidase (MAO) enzymes for the potential treatment of Alzheimer's disease (AD), is reported. Theoretical studies using 3D-Quantitative Structure-Activity ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2014, 75:82-95]

Cited: 42 times

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