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Author Isabel Iriepa

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Microscopic interactions between ivermectin and key human and viral proteins involved in SARS-CoV-2 infection.

Antonio Francés-Monerris, Cristina García-Iriepa, Isabel Iriepa, Cécilia Hognon, Tom Miclot, Giampaolo Barone, Antonio Monari, Marco Marazzi,

The identification of chemical compounds able to bind specific sites of the human/viral proteins involved in the SARS-CoV-2 infection cycle is a prerequisite to design effective antiviral drugs. Here we conduct a molecular dynamics study with the aim to assess the interactions of ivermectin, an antiparasitic drug with broad-spectrum antiviral ... Read more >>

Phys Chem Chem Phys (Physical chemistry chemical physics : PCCP)
[2021, 23(40):22957-22971]

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Privileged Quinolylnitrones for the Combined Therapy of Ischemic Stroke and Alzheimer's Disease.

José M Alonso, Alejandro Escobar-Peso, Alejandra Palomino-Antolín, Daniel Diez-Iriepa, Mourad Chioua, Emma Martínez-Alonso, Isabel Iriepa, Javier Egea, Alberto Alcázar, José Marco-Contelles,

Cerebrovascular diseases such as ischemic stroke are known to exacerbate dementia caused by neurodegenerative pathologies such as Alzheimer's disease (AD). Besides, the increasing number of patients surviving stroke makes it necessary to treat the co-occurrence of these two diseases with a single and combined therapy. For the development of new ... Read more >>

Pharmaceuticals (Basel) (Pharmaceuticals (Basel, Switzerland))
[2021, 14(9):]

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Studies on the affinity of 6-[(n-(cyclo)aminoalkyl)oxy]-4H-chromen-4-ones for sigma 1/2 receptors.

Winnie Deuther-Conrad, Daniel Diez-Iriepa, Isabel Iriepa, Francisco López-Muñoz, María Angeles Martínez-Grau, Michael Gütschow, José Marco-Contelles,

Sigma (σ) receptors represent attractive targets for the development of potential agents for the treatment of several disorders, including Alzheimer's disease and neuropathic pain. In the search for multitarget small molecules (MSMs) against such disorders, we have re-discovered chromenones as new affine σ<sub>1</sub>/σ<sub>2</sub> ligands. 6-(4-(Piperidin-1-yl)butoxy)-4<i>H</i>-chromen-4-one (<b>7</b>), a previously identified MSM ... Read more >>

RSC Med Chem (RSC medicinal chemistry)
[2021, 12(6):1000-1004]

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Tacrines as Therapeutic Agents for Alzheimer's Disease. V. Recent Developments.

Óscar M Bautista-Aguilera, Lhassane Ismaili, Isabel Iriepa, Daniel Diez-Iriepa, Fakher Chabchoub, José Marco-Contelles, Marta Pérez,

Herein we have reviewed our recent developments for the identification of new tacrine analogues for Alzheimer's disease (AD) therapy. Tacrine, the first cholinesterase inhibitor approved for AD treatment, did not stop the progression of AD, producing only some cognitive improvements, but exhibited secondary effects mainly due to its hepatotoxicity. Thus, ... Read more >>

Chem Rec (Chemical record (New York, N.Y.))
[2021, 21(1):162-174]

Cited: 1 time

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Homo-Tris-Nitrones Derived from α-Phenyl-N-tert-butylnitrone: Synthesis, Neuroprotection and Antioxidant Properties.

Daniel Diez-Iriepa, Beatriz Chamorro, Marta Talaván, Mourad Chioua, Isabel Iriepa, Dimitra Hadjipavlou-Litina, Francisco López-Muñoz, José Marco-Contelles, María Jesús Oset-Gasque,

Herein we report the synthesis, antioxidant and neuroprotective power of homo-tris-nitrones (<b>HTN</b>) <b>1-3</b>, designed on the hypothesis that the incorporation of a third nitrone motif into our previously identified homo-bis-nitrone <b>6</b> (<b>HBN6</b>) would result in an improved and stronger neuroprotection. The neuroprotection of <b>HTNs</b><b>1-3</b>, measured against oligomycin A/rotenone, showed that ... Read more >>

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

Cited: 3 times

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Thermodynamics of the Interaction between the Spike Protein of Severe Acute Respiratory Syndrome Coronavirus-2 and the Receptor of Human Angiotensin-Converting Enzyme 2. Effects of Possible Ligands.

Cristina García-Iriepa, Cécilia Hognon, Antonio Francés-Monerris, Isabel Iriepa, Tom Miclot, Giampaolo Barone, Antonio Monari, Marco Marazzi,

Since the end of 2019, the coronavirus SARS-CoV-2 has caused more than 1000000 deaths all over the world and still lacks a medical treatment despite the attention of the whole scientific community. Human angiotensin-converting enzyme 2 (ACE2) was recently recognized as the transmembrane protein that serves as the point of ... Read more >>

J Phys Chem Lett (The journal of physical chemistry letters)
[2020, 11(21):9272-9281]

Cited: 2 times

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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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Thermodynamics of the interaction between the spike protein of severe acute respiratory syndrome- coronavirus-2 and the receptor of human angiotensin converting enzyme 2. Effects of possible ligands

Cristina Garcia-Iriepa, Cecilia Hognon, Antonio Francés-Monerris, Isabel Iriepa, Tom Miclot, Giampaolo Barone, Antonio Monari, Marco Marazzi,

Since the end of 2019, the coronavirus SARS-CoV-2 has caused more than 180,000 deaths all over the world, still lacking a medical treatment despite the concerns of the whole scientific community. Human Angiotensin-Converting Enzyme 2 (ACE2) was recently recognized as the transmembrane protein serving as SARS-CoV-2 entry point into cells, ... Read more >>

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Synthesis, antioxidant properties and neuroprotection of α-phenyl-tert-butylnitrone derived HomoBisNitrones in in vitro and in vivo ischemia models.

Beatriz Chamorro, Daniel Diez-Iriepa, Belén Merás-Sáiz, Mourad Chioua, David García-Vieira, Isabel Iriepa, Dimitra Hadjipavlou-Litina, Francisco López-Muñoz, Ricardo Martínez-Murillo, Daniel Gonzàlez-Nieto, Israel Fernández, José Marco-Contelles, María Jesús Oset-Gasque,

We herein report the synthesis, antioxidant power and neuroprotective properties of nine homo-bis-nitrones HBNs 1-9 as alpha-phenyl-N-tert-butylnitrone (PBN) analogues for stroke therapy. In vitro neuroprotection studies of HBNs 1-9 against Oligomycin A/Rotenone and in an oxygen-glucose-deprivation model of ischemia in human neuroblastoma cell cultures, indicate that (1Z,1'Z)-1,1'-(1,3-phenylene)bis(N-benzylmethanimine oxide) (HBN6) is ... Read more >>

Sci Rep (Scientific reports)
[2020, 10(1):14150]

Cited: 2 times

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Triazolopyridopyrimidine: A New Scaffold for Dual-Target Small Molecules for Alzheimer's Disease Therapy.

Lazhar Zribi, Irene Pachòn-Angona, Òscar M Bautista-Aguilera, Daniel Diez-Iriepa, José Marco-Contelles, Lhassane Ismaili, Isabel Iriepa, Fakher Chabchoub,

Alzheimer's disease (AD) is multifactorial disease characterized by the accumulation of abnormal extracellular deposits of amyloid-beta (Aβ) peptide, and intracellular neurofibrillary tangles (NFTs), along with dramatic neuronal death and decreased levels of choline acetyltransferase. Given the limited therapeutic success of available drugs, it is urgent to explore all the opportunities ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2020, 25(14):]

Cited: 0 times

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Acetylcholinesterase Inhibition of Diversely Functionalized Quinolinones for Alzheimer's Disease Therapy.

Óscar M Bautista-Aguilera, Lhassane Ismaili, Mourad Chioua, Rudolf Andrys, Monika Schmidt, Petr Bzonek, María Ángeles Martínez-Grau, Christopher D Beadle, Tatiana Vetman, Francisco López-Muñoz, Isabel Iriepa, Bernard Refouvelet, Kamil Musilek, José Marco-Contelles,

In this communication, we report the synthesis and cholinesterase (ChE)/monoamine oxidase (MAO) inhibition of 19 quinolinones (<b>QN1</b>-<b>19</b>) and 13 dihydroquinolinones (<b>DQN1</b>-<b>13</b>) designed as potential multitarget small molecules (MSM) for Alzheimer's disease therapy. Contrary to our expectations, none of them showed significant <i>human recombinant</i> MAO inhibition, but compounds <b>QN8</b>, <b>QN9</b>, and ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2020, 21(11):]

Cited: 0 times

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Chromenones as Multineurotargeting Inhibitors of Human Enzymes.

Carina Lemke, Joscha Christmann, Jiafei Yin, José M Alonso, Estefanía Serrano, Mourad Chioua, Lhassane Ismaili, María Angeles Martínez-Grau, Christopher D Beadle, Tatiana Vetman, Florian M Dato, Ulrike Bartz, Paul W Elsinghorst, Markus Pietsch, Christa E Müller, Isabel Iriepa, Timo Wille, José Marco-Contelles, Michael Gütschow,

The complex nature of multifactorial diseases, such as Morbus Alzheimer, has produced a strong need to design multitarget-directed ligands to address the involved complementary pathways. We performed a purposive structural modification of a tetratarget small-molecule, that is contilisant, and generated a combinatorial library of 28 substituted chromen-4-ones. The compounds comprise ... Read more >>

ACS Omega (ACS omega)
[2019, 4(26):22161-22168]

Cited: 2 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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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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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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Novel Quinolylnitrones Combining Neuroprotective and Antioxidant Properties.

Mourad Chioua, Manuel Salgado-Ramos, Daniel Diez-Iriepa, Alejandro Escobar-Peso, Isabel Iriepa, Dimitra Hadjipavlou-Litina, Emma Martínez-Alonso, Alberto Alcázar, José Marco-Contelles,

We describe here the preparation, neuroprotective analysis, and antioxidant capacity of 11 novel quinolylnitrones (QN). The neuroprotective analysis of QN1-11 in an oxygen-glucose deprivation model, in primary neuronal cultures, has been determined, allowing us to identify QN6 as a very potent neuroprotective agent, showing significant high value at 0.5 and ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2019, 10(6):2703-2706]

Cited: 6 times

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Synthesis, neuroprotective and antioxidant capacity of PBN-related indanonitrones.

Alicia Jiménez-Almarza, Daniel Diez-Iriepa, Mourad Chioua, Beatriz Chamorro, Isabel Iriepa, Ricardo Martínez-Murillo, Dimitra Hadjipavlou-Litina, María Jesús Oset-Gasque, José Marco-Contelles,

In this work six PBN-related indanonitrones 1-6 have been designed, synthesized, and their neuroprotection capacity tested in vitro, under OGD conditions, in SH-SY5Y human neuroblastoma cell cultures. As a result, we have identified indanonitrones 1, 3 and 4 (EC<sub>50</sub> = 6.64 ± 0.28 μM) as the most neuroprotective agents, and in particular, among them, indanonitrone ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2019, 86:445-451]

Cited: 4 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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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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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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