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Menu
  • Home
  • Research overview
    • Medicinal Chemistry and Chemical Biology of GPCRs
    • Development of novel multicomponent-based synthetic strategies
    • Design and optimization of novel heterogeneous catalysts by 3D printing
    • ComBioMed platform for drug discovery
  • Group members
  • Eddy
  • Publications
  • Doctoral Theses
  • Financial Support
  • News
  • Research opportunities

Publications

2022
2021
2020
2019
2018
2017
2016
2015
2014
2013
2012
2011
2010-2005
2005-
2022

Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations

Willem Jespers, Laura H. Heitman, Adriaan P. IJzerman, Eddy Sotelo, Gerard J. P. van Westen, Johan Åqvist, Hugo Gutie ́rrez-de-Tera ́n

PLOS Computational Biology., 2021, 17, e1009152

https://journals.plos.org/ploscompbiol/article?id=10.1371/journal.pcbi.1009152

 


A2B adenosine receptor antagonists rescue lymphocyte activity in adenosine-producing patient-derived cancer models

Apple Hui Min Tay, Rubén Prieto-Díaz, Shiyong Neo, Le Tong, Xinsong Chen, Valentina Carannante, Björn Önfelt, Johan Hartman, Felix Haglund, Maria Majellaro, Jhonny Azuaje, Xerardo Garcia-Mera, Jose M Brea, Maria I Loza, Willem Jespers, Hugo Gutierrez-de-Teran, Eddy Sotelo, Andreas Lundqvist

J. Immunother Cancer, 2022, 10, e004592

https://jitc.bmj.com/content/10/5/e004592

 


Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent GPCR ligands

Identification of A2BAR as a potential target in colorectal cancer using novel
fluorescent GPCR ligands

J. Barbazan, M. Majellaro, A. L. Martínez, J. M. Brea, E. Sotelo, M. Abal

Biomedicine & Pharmacotherapy 2022;153, 113408

https://www.sciencedirect.com/science/article/pii/S0753332222007971 


Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective A1 Antagonists

Cristina Val, Carlos Rodríguez-García, Rubén Prieto-Díaz, Abel Crespo, Jhonny Azuaje, Carlos Carbajales, Maria Majellaro, Alejandro Díaz-Holguín, José M. Brea, Maria Isabel Loza, Claudia Gioé-Gallo, Marialessandra Contino, Angela Stefanachi, Xerardo García-Mera, Juan C. Estévez, Hugo Gutiérrez-de-Terán and Eddy Sotelo

J. Med. Chem. 2022, 63, 2091-2116.

https://doi.org/10.1021/acs.jmedchem.1c01636

 


Exploring Non-orthosteric Interactions with a Series of Potent and Selective A3 Antagonists

Darío Miranda-Pastoriza, Rodrigo Bernárdez, Jhonny Azuaje, Rubén Prieto-Díaz, Maria Majellaro, Ashish V. Tamhankar, Lucien Koenekoop, Alejandro González, Claudia Gioé-Gallo, Ana Mallo-Abreu, José Brea*, M. Isabel Loza, Aitor García-Rey, Xerardo García-Mera, Hugo Gutiérrez-de-Terán*, and Eddy Sotelo*

ACS Med. Chem. Lett. 2022, 13, 243-249.

https://doi.org/10.1021/acsmedchemlett.1c00598

 


2021
Similarities and differences upon binditng of naturally occurring Δ9-tetrahydrocannabinol-derivatives to cannabinoid CB1 and CB2 receptors

RaichIu Raich, Rafael Rivas-Santisteban, Alejandro Lillo, Jaume Lillo, Irene Reyes-Resina, Xavier Nadal, Carlos Ferreiro-Vera, Verónica Sánchez de Medina, Maria Majellaro, Eddy Sotelo, Gemma Navarro, Rafael Franco

 

Pharmacological Research, 2021, 174, 105970

https://doi.org/10.1016/j.phrs.2021.105970

 


Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition
Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagon…
Xuesong Wang, Willem Jespers, Rubén Prieto-Díaz, Maria Majellaro, Adriaan P IJzerman, Gerard JP van Westen, Eddy Sotelo, Laura H Heitman, Hugo Gutiérrez-de-Terán

 

Scientific Reports volume 11, Article number: 14171 (2021)

https://doi.org/10.1038/s41598-021-93419-x

 

 

 

 

 

 


Potent and Subtype-Selective Dopamine D2 Receptor Biased Partial Agonists Discovered via an Ugi-Based Approach

Ana Mallo-Abreu, Irene Reyes-Resina, Jhonny Azuaje, Rafael Franco, Aitor García-Rey, Maria Majellaro, Darío Miranda-Pastoriza, Xerardo García-Mera, Willem Jespers, Hugo Gutiérrez-de-Terán,
Gemma Navarro, and Eddy Sotelo*

 

J. Med. Chem. 2021, 64, 8710-8726

https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c00704


Catalytic performance of a metal-free graphene oxide-Al2O3 composite assembled by 3D printing

JhonnyAzuaje, AdriánRama, AnaMallo-Abreu, Mónica G.Boado, MaríaMajellaro, Carmen R.Tubío, RubénPrieto, XerardoGarcía-Mera, FranciscoGuitián, EddySotelo, AlvaroGil

Journal of the European Ceramic Society, 2021, Volume 41, Issue 2, 1399-1406  https://doi.org/10.1016/j.jeurceramsoc.2020.10.010


3,4-Dihydropyrimidin-2(1H)-ones as Antagonists of the Human A2B Adenosine Receptor: Optimization, Structure–Activity Relationship Studies, and Enantiospecific Recognition

María Majellaro, Willem Jespers, Abel Crespo, María J. Núñez, Silvia Novio, Jhonny Azuaje, Rubén Prieto-Díaz, Claudia Gioé, Belma Alispahic, José Brea*, María I. Loza, Manuel Freire-Garabal, Carlota Garcia-Santiago, Carlos Rodríguez-García, Xerardo García-Mera, Olga Caamaño, Christian Fernandez-Masaguer, Javier F. Sardina, Angela Stefanachi, Abdelaziz El Maatougui, Ana Mallo-Abreu, Johan Åqvist, Hugo Gutiérrez-de-Terán*, and Eddy Sotelo*

J. Med. Chem. 2021, 64, 1, 458–480, https://doi.org/10.1021/acs.jmedchem.0c01431


2020
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A2B Adenosine Receptor Antagonists

Ana Mallo-Abreu, Rubén Prieto-Díaz, Willem Jespers, Jhonny Azuaje, Maria Majellaro, Carmen Velando, Xerardo García-Mera, Olga Caamaño, José Brea, María I. Loza, Hugo Gutiérrez-de-Terán, and Eddy Sotelo

Journal of Medicinal Chemistry, 2020, 63, 7721-7739. https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00564


X‐Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A2A Adenosine Receptor Antagonists

Willem Jespers, Grégory Verdon, Jhonny Azuaje, Maria Majellaro, Henrik Keränen,† Xerardo García-Mera, Miles Congreve, Francesca Deflorian, Chris de Graaf, Andrei Zhukov, Andrew S. Doré, Jonathan S. Mason, Johan Åqvist,Robert M. Cooke, Eddy Sotelo and Hugo Gutiérrez-de-Terán

Angew. Chem. Int. Ed., 2020, 59 https://doi.org/10.1002/anie.202003788


The European Research Network on Signal Transduction (ERNEST): Toward a Multidimensional Holistic Understanding of G Protein- Coupled Receptor Signaling

Martha E. Sommer, Jana Selent, Jens Carlsson, Chris De Graaf, David E. Gloriam, Gyorgy M. Keseru, Mickey Kosloff, Stefan Mordalski, Aurelien Rizk, Mette M. Rosenkilde, Eddy Sotelo, Johanna K. S. Tiemann, Andrew Tobin, Nina Vardjan, Maria Waldhoer, and Peter Kolb

ACS Pharmacol. Transl. Sci. 2020, 3, 2, 361–370. https://pubs.acs.org/doi/10.1021/acsptsci.0c00024


2019
Trifluorinated Pyrimidine-Based A2B Antagonists: Optimization and Evidence of Stereospecific Recognition

Ana Mallo-Abreu, María Majellaro, Willem Jespers, Jhonny Azuaje, Olga Caamaño, XerardoGarcía-Mera, José M.Brea, MaríaI.Loza, HugoGutieŕrez-de-Terań,
and Eddy Sotelo

J. Med. Chem. 2019, 62, 9315−9330 https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01340


Free-Energy Calculations for Bioisosteric Modifications of A3 Adenosine Receptor Antagonists

Zuzana Jandova, Willem Jespers, Eddy Sotelo, Hugo Gutiérrez-de-Terán and Chris Oostenbrink

Int. J. Mol. Sci. 2019, 20(14), 3499 https://www.mdpi.com/1422-0067/20/14/3499


2018

Clinical validation of blood/brain glutamate grabbing in acute ischemic stroke.

Silva, A., Pérez-Díaz, A., Santamaría, M., Correa-Paz, C., Rodríguez-Yáñez, M., Ardá, A., Pérez-Mato, M., Iglesias-Rey, R., Brea, J., Azuaje, J., Sotelo, E., Sobrino, T., Loza, M., Castillo, J., Campos, F

Annals of Neurology, 2018, 84, 260-273. https://doi.org/10.1002/ana.25286


Structural Mapping ogf Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms.

Jespers, W., Schiedel, A. C., Heitman, L., Cooke, R., Leene, L., van Westen, G. J., Glorian, D. E., Muller, C. E., Sotelo, E., Gutiérrez de Terán, H.

Trends in Pharmacological Sciences, 2018, 39, 75-89. https://doi.org/10.1016/j.tips.2017.11.001


Three-Dimensional Printing in Catalysis: Combining 3D Heterogeneous Copper and Palladium Catalysts for Multicatalytic Multicomponent Reactions

Díaz-Marta, A.S. Tubío, C.R., Carbajales, C., Fernandez, C., Escalante, L., Sotelo, E., Guitián, F., Barrio, V. L., Gil, A., Coelho, A.

ACS Catalysis. 2018, 8, 392-404 https://pubs.acs.org/doi/abs/10.1021/acscatal.7b02592


2017

Development of Fluorescent Probes that Target Serotonin 5HT2B receptors

Azuaje, J., López, Paula, Iglesias, A., De la Fuente, R., Pérez-Rubio, J. M., García, D., Pérez, D., Stepniewski, T., García-Mera, X., Loza, M. I., Cadavid, M. I. Brea, J., Sotelo, E.*

Scientific Reports. 2017, 7, 11370-3. https://www.nature.com/articles/s41598-017-11370-2


Effect of Nitrogen Atom Substitution in A3 Adenosine Receptor Binding: N(4,6-Dirarylpyridin-2-yl)acetamides as Potent and Selective Antagonists

Azuaje, J., Jespers, W., Yaziji, V., Mallo, A., Majellaro, M., Caamaño, O., Loza, M. I., Cadavid, M. I. Brea, J. Gutiérrez de Terán, H., Sotelo, E.*

Journal of Medicinal Chemistry, 2017, 60, 7502-7511. https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.7b00860


3-Oxopyridazin-5-yl-Chalcone Hybrids: Potent Antiplatelet Agents that Prevent GP IIb/IIIa Activation

El Maatougui, A., Yañez, M., Crespo, A., Fraiz, N., Coelho, A., Raviña, E., Cano, E., Loza, M. I., Brea, J., Gutiérrez de Terán, H., Sotelo, E.*

ChemistrySelect, 2017, 2, 4920-4933. https://onlinelibrary.wiley.com/doi/10.1002/slct.201700243


Synthesis and Characterization of a New Bivalent Ligand Combining Caffeine and Docosahexaenoic Acid

Fernandez-Dueñas, V., Morato, X., Ciruela, F., Azuaje, J., Sotelo, E.* Cordobilla, B., Domingo, J.C.

Molecules. 2017, 22, 3661-11. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155394/


Enantiospecific Recognition at the A2B Adenosine Receptor by Alkyl 2-Cyanoimino-4-substituted-6-methyl-1,2,3,4-tetrahydropyrimiidine-5-carboxylates

Carbajales, C., Azuaje, J., Oliveira, A., Loza, M.I., Brea, J., Cadavid, M.I., Masaguer, C. F., García-Mera, X., Gutiérrez de Terán, H., Sotelo, E.*

Journal of Medicinal Chemistry. 2017, 60, 3372-3382. https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.7b00138


An Efficient and Recyclable 3D Printed α-Al2O3 Catalyst for the Multicomponent Assembly of Bioactive Heterocycles

Azuaje, J., Tubio, C.R., Escalante, L., Gomez, M., Coelho, A., Caamaño, O., Gil, A., Sotelo, E.*

Applied Catalysis, A: General, 2017, 530, 203-210. https://www.sciencedirect.com/science/article/pii/S0926860X16305701


Multicomponent Assembly of the Kinesin Spindle Protein Inhibitor CPUYJ039 and Analogues as Antimitotic Agents.

Carbajales, C., Sawada, J-C., Marzano, G., Sotelo, E., Escalante, L., Sanchez-Diaz Marta, A., García-Mera, X., Asai, A., Coelho, A.

ACS Comb. Sci. 2017, 19, 153-160. https://pubs.acs.org/doi/abs/10.1021/acscombsci.6b00166


Structure-Based Rational Design of Adenosine Receptor Ligands.

Gutiérrez-de-Terán, H. Sallander, J. Sotelo, E.

Current Topics In Medicinal Chemistry, 2017, 17, 40-58. https://www.ingentaconnect.com/contentone/ben/ctmc/2017/00000017/00000001/art00007


2016

Drug Structural Features Affect Drug Delivery from Hyperbranched Polyesteramide Hot Melt Extrudates.

Raviña-Eirín, E., Azuaje, J., Sotelo, E. Gómez-Amoza, J. L., Martínez-Pacheco, R.

European Journal of Pharmaceutics and Biopharmaceutics, 2016, 102, 1-78. https://www.sciencedirect.com/science/article/pii/S0939641116300108


Discovery of Potent and Highly Selective Adenosine A2B Receptor Antagonists Chemotypes.

El Maatougi, A., Azuaje, J., González-Gómez, M., Míguez, G., Crespo, A., García-Mera, X.,  Gutiérrez de Terán, H., Sotelo, E.*

Journal of Medicinal Chemistry, 2016, 59, 1967-1983. https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b01586


3D-Printing of a Heterogeneous Copper-Based Catalyst

Tubio, C. R., Azuaje, J., Escalante, L., Coelho, A., Sotelo, E. Gil, A.

Journal of Catalysis, 2016, 334, 110-115. https://www.sciencedirect.com/science/article/pii/S0021951715003838


2015

Pyrazin-2(1H)-ones as a Novel Class of Selective A3 Adenosine Receptor Antagonists.

Azuaje, J., Carbajales, C, González-Gomes, M., Coelho, A., Caamaño, O., Gutierrez de Terán, H., Sotelo, E.

Future Medicinal Chemistry, 2015, 7, 1373-1380. https://www.future-science.com/doi/10.4155/fmc.15.69


Sol-Gel Entrapped Cu in Silica Matrix: An Efficienct Heterogeneous Nanocatalyst For Huisgen, and Ullmann Reactions.

Diz, P., Gil, A., Guitían, F., El Maatougui, A., Azuaje, J., Pernas, P., Sotelo, E., Coelho, A.

Applied Catalysis A: General  , 2015, 502, 86-95. https://www.sciencedirect.com/science/article/pii/S0926860X1530003X


Integrated Ugi-Based Assembly of Functional, Skeletal and Stereochemically Diverse 1,4-Benzodiazepin-2-ones.

Azuaje, J., Pérez-Rubio, J. M., Yaziji, V., El Maatougui, González-Gómez, J. C., Masaguer, C. F., Sánchez-Pedregal, V., Navarro-Vázquez, A., Teijeira, M., Sotelo, E.*

J. Org. Chem. 2015, 80, 1533-1549. https://pubs.acs.org/doi/abs/10.1021/jo502382q


Computer-Aided Design of GPCR Ligands.

Gutiérrez-de-Terán, H., Keranen, H., Azuaje, J., Rodriguez, D., Sotelo, E.

Methods in Molecular Biology, 2015, 1272, 1272-1291. https://link.springer.com/protocol/10.1007%2F978-1-4939-2336-6_19


2014

Structure-Based Design of Novel KSP-Eg5 Inhibitors Assisted by a Targeted Multicomponent Reaction.

Carbajales, C., Prado, M. A., Gutiérrez-de-Terán, H., Cores, A., Azuaje, J., Novio, S., Nuñez, M. J., Fernández, B., Sotelo, E., García-Mera, X., Sánchez-Lazo, P., Freire-Garabal, M., Coelho, A.

 

 

 

ChemBioChem, 2014, 15, 1471-1480. https://onlinelibrary.wiley.com/doi/full/10.1002/cbic.201402089

 

 

 


Ugi-Based Approaches to Quinoxaline Libraries.

Azuaje, J., El Maatougui, García-Mera, X., Sotelo, E.*

ACS Combinatorial Science, 2014, 16, 403-411. https://pubs.acs.org/doi/abs/10.1021/co500036n


2013

Discovery of 3,4-Dihydropyrimidin-2(1H)-ones as a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists.

Crespo, A., El Maatougui, A.,Biagini, P., Azuaje, J., Coelho, A., García-Mera, X., Brea, J., Loza, M. I., Cadavid, M. I., Sotelo, E.*

ACS Medicinal Chemistry Letters, 2013, 4, 1031-1036. https://pubs.acs.org/doi/10.1021/ml400185v


Copper-Catalyzed Huisgen 1,3-Dipolar Cycloaddition Under Oxidative Conditions: Polymer-Assisted Assembly of 4-Acyl-1-Substituted-1,2,3-Triazoles

Diz, P., Coelho, A., El Maatougui, A., Azuaje, J., Caamaño, O., Gil, A., Sotelo, E.*

The Journal of Organic Chemistry, 2013, 78, 6540-6549. https://pubs.acs.org/doi/10.1021/jo400800j


Three-Component Assembly of Structurally Diverse 2-Aminopyrimidine-5-carbonitriles.

Val, C., Crespo, A., El Maatougui, A., Azuaje, J. A., Coelho, A., Sotelo, E.*

ACS Comb. Sci., 2013, 15, 370-378. https://pubs.acs.org/doi/abs/10.1021/co4000503


Multicomponent Assembly of Diverse Pyrazin-2(1H)-one Chemotypes

Azuaje, J., El Maatougui, A., Pérez-Rubio, J. M., Coelho, A., Fernández, F. Sotelo, E.*

The Journal of Organic Chemistry, 2013, 78, 4402-4409. https://pubs.acs.org/doi/abs/10.1021/jo4003163


Selective and potent Adenosine A3 Receptor Antagonists by Methoxyaryl Substitution on the N-(2,6-Diarylpyrimidin-4-yl)acetamide scaffold.

Yaziji, V., Rodríguez, D., Gutiérrez de Terán, H., Coelho, A., El Maatougui, A., Brea, J., Loza, M. I., Garcia-Mera, X., Cadavid, M.I., Sotelo, E.*

European Journal of Medicinal Chemistry. 2013, 59, 235-242. https://www.sciencedirect.com/science/article/pii/S0223523412006794


2012

Discovery and Preliminary SAR of 5-Arylidene-2,2,-dimethyl-1,3-dioxane-2,4-diones as Platelet Aggregation Inhibitors.

El Maatougui, A., Azuaje, J., Coelho, A., Cano, E., Yañez, M., Yaziji, V., Carbajales, C., Sotelo, E.*

Combinatorial Chemistry & High Throughput Screening, 2012, 15, 551-554. http://www.eurekaselect.com/100357


2011

Pyrimidine Derivatives as Potent and Selective A3 Adenosine Receptor Antagonists.

. Yaziji, V., Rodríguez, D., Gutiérrez de Terán, H., Coelho, A., Brea, J., Loza, M. I., Garcia-Mera, X., Cadavid, M.I., Caamaño, Sotelo, E.*

Journal of Medicinal Chemistry. 2011, 54, 457-471. https://pubs.acs.org/doi/abs/10.1021/jm100843z


Supported Tosic Acid as Highly Robust and Eco-Friendly Isocyanide´s Scavengers.

Azuaje, J., Al Maatougui, A., Blanco, J.M., Coelho, A., Sotelo, E.*

ACS Combinatorial Science, 2011, 13, 89-95. https://pubs.acs.org/doi/10.1021/co100035z


Silica-Supported Aluminum Chloride-Assisted Solution Phase Synthesis of Pyridazinone-Based Antiplatelet Agents.

El Maatougui, A., Azuaje, J., Sotelo, E., Caamaño, O., Coelho, A.

ACS Combinatorial Science 2011, 13, 7-12. https://pubs.acs.org/doi/abs/10.1021/co100017h


Convergent Assembly of Structurally Diverse Quinazolines.

Crespo, A., Coelho, A., Diz, P., Fernández, F., Novoa de Armas, H., Sotelo, E.*

Organic & Biomolecular Chemistry, 2011, 9, 351-357. https://pubs.acs.org/doi/abs/10.1021/co100017h


2010-2005

Polymer Supported 1,5,7-triazabicylo[4,4,0]dec-5-ene as Polyvalent Ligands in the Copper Catalysed Huisgen 1,3-Dipolar Cycloaddition.

Coelho, A., Díz, P., Caamaño, O., Sotelo, E.*

Advanced Synthesis & Catalysis, 2010, 352, 1179-1192. https://onlinelibrary.wiley.com/doi/10.1002/adsc.200900680


Divergent Solution Phase Synthesis of Diarylpirimidines as Selective A3 Adenosine Receptor Antagonsits

Yaziji, V., Coelho, A., El Maatougui, Brea, J., Loza, M. I., Garcia-Mera, X., Sotelo, E.*

Journal of Combinatorial Chemistry, 2009, 11, 519-522. https://pubs.acs.org/doi/10.1021/cc900044k


Synthetic Applications of Polystyrene 1,1,3,3-Tetramethylguanidine

Coelho, A., Crespo, A., Fernández, F., Biagini, P., Stefanachi, A., Sotelo, E.*

Combinatorial Chemistry & Highthroughput Screening, 2008, 11, 843-847. http://www.eurekaselect.com/68075


Click Chemistry Approach to Assembly Proline Mimetic Libraries Containing 1,4-Substituted 1,2,3-Triazoles.

Rodriguez-Borges, J. E., Gonçalves, S., do Vale, M. L., García-Mera, X., Coelho, A., Sotelo, E.

Journal of Combinatorial Chemistry, 2008, 10, 372-375. https://pubs.acs.org/doi/10.1021/cc800035z


Design, Synthesis and Biological Evaluation of Glycine-Based Molecular Tongs as Inhibitors of α-β 1-40 Aggregation in Vitro.

Cellamare, S., Stefanachi, A., Antonella, S., Basile, T., Catto, M., Campagna, F., Sotelo, E., Carotti, A.

Bioorganic & Medicinal Chemistry, 2008, 16, 4810-4822. https://www.sciencedirect.com/science/article/pii/S096808960800271X


1,3- and 8-Substituted-9-Deazaxanthines as Potent and Selective Antagonists at the Human A2B Adenosine Receptor

Stefanachi, A., Brea, J. M., Cadavid M. I., Centeno, N. B., Esteve, C., Loza, M. I., Martínez, A., Nieto, R., Raviña, E., Sanz, F., Segarra, V., Sotelo, E., Vidal, B., Carotti, A.

Bioorganic & Medicinal Chemistry, 2008, 16, 2852-2859. https://www.sciencedirect.com/science/article/pii/S0968089608000035


2-Substituted 4-, 5- and 6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones and 2-Substituted 4,5-bis[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones as Potent Platelet Aggregation Inhibitors: Design, Synthesis and SAR Studies.

Meyers, C., Yáñez, M., Elmatougi, A., Verhest, T., Coelho, A., Fraiz, N., Lemière, G. L. F., García-Mera, X., Laguna, R., Cano, E., Maes, B. U. W., Sotelo, E.*

Bioorganic & Medicinal Chemistry Lett. 2008, 18, 793-797. https://www.sciencedirect.com/science/article/pii/S0960894X07013431


Synthesis, Adenosine Receptor Binding and 3D-QSAR- of 4-Substituted 2-(2´-furyl)-1,2,4-triazolo[1,5-a]quinoxalines.

Martínez A., Gutierrez de Terán, H., Brea, J. M., Raviña, E., Loza, M. I., Cadavid, M. I., Sanz, F., Segarra, V., Vidal, B. Sotelo, E.*

Bioorganic & Medicinal Chemistry, 2008, 16, 2103-2113. https://www.sciencedirect.com/science/article/pii/S0968089608000515


Design, Synthesis and Structure Activity Relationships of a Novel Series of 5-Alkylidenenpyridazin-3-ones with a non c-AMP-Based Antiplatelet Activity.

Coelho, A., Raviña, E., Yáñez, M., Fraiz, N., Laguna, R., Cano, E., Sotelo, E.*

Journal of Medicinal Chemistry, 2007, 50, 6476-6484. https://pubs.acs.org/doi/10.1021/jm061401d


Parallel Regulation By Olanzapine Of The Patterns Of Expression Of 5-Ht2a And D3 Receptors In Rat Central Nervous System And Blood Cells.

Padín; J. F., Rodríguez; M.A., Domínguez; E., Dopeso-Reyes; I. G., Buceta; M., Cano; E., Sotelo, E., Caruncho; H. J., Cadavid; M. I., Castro; M., Loza, M.I.

Neuropharmacology, 2006, 51, 923-932. https://www.sciencedirect.com/science/article/pii/S0028390806001882


2005-

Expanding the Chemical Diversity of Azinone Libraries by A Consecutive Alkylation/Palladium-Catalysed Functionalization Strategy

Coelho, A., Sotelo, E.*

Journal of Combinatorial Chemistry, 2005, 7, 526-529. https://pubs.acs.org/doi/10.1021/cc050036t


Reactivity of 5-Alkynylpyridazinones Toward Hydrochloric Acid

Coelho, A., Novoa, H., Peeters, O.M., Blaton, N., Sotelo, E.*

Tetrahedron, 2005, 61, 4785-4791. https://www.sciencedirect.com/science/article/pii/S004040200500428X


Reactivity of 5-Iodopyridazin-3(2H)-ones in Palladium-Catalysed Reactions

Coelho, A., Sotelo, E., Novoa, H., Peeters, O.M., Blaton, N., Raviña, E.

Tetrahedron, 2004, 60, 12177-12189. https://www.sciencedirect.com/science/article/pii/S0040402004016941


8-Substituted-9-deazaxanthines as Adenosine Receptor Ligands: Design, Synthesis and Structure-affinity Relationships at A2B

Carotti, A., Stefanachi, A., Raviña, E., Sotelo, E., Loza, M. I., Cadavid, M. I., Centeno, N. B.

European Journal of Medicinal Chemistry, 2004, 39, 879-887. https://www.sciencedirect.com/science/article/pii/S0223523404001618


Efficient Heck Alkenylation at position 5 of the 6-phenyl-3(2H)-pyridazinone System.

Coelho, A., Sotelo, E., Novoa, H., Blaton, N., Peeters, O.M., Raviña, E.

Tetrahedron Letters, 2004, 45, 3459-3463. https://www.sciencedirect.com/science/article/pii/S004040390400509X


Facile Solution Phase Combinatorial Synthesis of Highly Substituted Pyridazinones

Sotelo, E.*

Molecular Diversity 2004, 8, 159-163. https://link.springer.com/article/10.1023/B%3AMODI.0000025628.01102.81


Stille-Based Approaches in the Synthesis of 6-phenyl-5-Substituted-3(2H)-pyridazinones.

Sotelo, E., Coelho, A., Raviña, E.

Chem. Pharm. Bull., 2003, 5, 427-430. https://www.jstage.jst.go.jp/article/cpb/51/4/51_4_427/_pdf


Sonogashira Approaches in The Synthesis of 5-Substituted-6-phenyl-3(2H)-pyridazinones.

Coelho, A., Sotelo, E., Raviña, E.

Tetrahedron, 2003, 59, 2477-2484. https://www.sciencedirect.com/science/article/pii/S0040402003002631


Retro-Ene-Assisted Palladium-Catalysed Synthesis of 4,5-Disubstituted-3(2H)-pyridazinones.

Sotelo, E., Coelho, A., Raviña, E.

Tetrahedron Lett., 2003, 44, 4459-4462. https://www.sciencedirect.com/science/article/pii/S0040403903010293


Traceless Solid Phase Synthesis of 4,5- and 5,6-Diaryl-3(2H)-pyridazinones.

Sotelo, E., Raviña, E.

Synlett, 2003, 1113-1116. https://www.thieme-connect.com/products/ejournals/pdf/10.1055/s-2003-39882.pdf


ComBioMed Research Group
Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS) y Departamento de Química Orgánica. Facultad de Farmacia.
Universidad de Santiago de Compostela. Campus Vida. 15782.
Santiago de Compostela. Spain.
Tel. 881 815732
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