History UAH 1

Although our research group, HETEROBETAINES, has been continuously developing its research at the University of Alcalá since 1985, and it has been also involved into an interdisciplinary Master program for graduates in Chemistry and Pharmacy. The funding requested in the present Project aims to achieve a general restructuring of the group, making use of our experience and acquired knowledge, but trying a more intense internationalization, to capture young talent and promoting the interdisciplinary work that already characterizes us. All aspects adapting to the Spanish Strategy of Science, Technology and Innovation integrated in Horizon 2020. As a continuation of the Projects underway, our most immediate targets would be centered either to the development of new methodologies in the preparation of heterocyclic systems, or to the use of them to the preparation of bioactive compounds useful in the field of diagnosis, all of them with heterocyclic structure.

Innovation in the pharmaceutical industry is a complex phenomenon that makes an important contribution to the welfare and health status of the society, involving different agents (academics, industry, patients, doctors, governments, international organizations), and whose influence is not restricted to the pharmaceutical sector, but it is crucial for the economy as a whole. HETEROBETAINES has always been characterized as a Medicinal Chemistry group, with extensive collaborations with the pharmaceutical industry, working with companies such as LILLY, SERVIER, ALMIRALL etc, and the philosophy of the Group has always been to acquire the necessary knowledge to build molecules, with high added value, that could be applied in the field of Medicinal Chemistry, either as bioactive molecules or as dyes, fluorescent markers, or PET reagents of biomedical use.

The research team of this project has taken an active part in the development of undergraduate studies in Pharmacy and in various related master and doctoral programs. It can also be noted that some of the professors have been involved in the creation of the first Pilot Plant facility for scaling up drug synthesis in a Spanish university (CQAB, University of Alcalá).

Points to consider

The Project Research Team is teaching staff of a Master in Drug Discovery and a PhD in MEDICINAL CHEMISTRY (MCD 2005 00083) (http://www.quimed.org) with Mention of Quality during the years 2005-2010 and distinguished with Mention towards Excellence by the Ministry of Education, courses 2011-2015 (Reference: MEE2011-0415). It should also be pointed out that practically 100% of our doctors find a stable job, mainly in the pharmaceutical industry (currently in LILLY SA, JANSSEN, GLAXO SK, PHARMAMAR, ALTER, SYNTHETIC CHEMISTRY, VILLALFARMA and MERCK S&D) or they continue his training process through post-doctoral stays (2-5 years).

The PhD program is integrated into the European Ph.D. network of Medicinal Chemistry, Paul Ehrlich European Medicinal Chemistry Ph.D. Network http://www.pehrlichmedchem.eu. This network facilitates the mobility of students and teachers within the network, so that, for example, the students of this doctorate can make short stays (3 months) in one of the groups of the network and in turn they do postdoctoral stays once completed his Doctoral Thesis.

See now some projects of the last five years, in which our researchers participate or have participated: DOWNLOAD HERE

Members

Carolina Burgos García was born in Segovia in 1962. She obtained a Doctorate in Pharmacy at the Organic Chemistry Department of the University of Alcalá in 1991, working under the direction of Profs Enrique Gálvez and Mª Luisa Izquierdo. In 1991 he made a post-doctoral stay at the Laboratorios ALTER S.A, with a grant from the OPIS plan to transfer doctors to the Pharmaceutical Industry, where he worked under the direction of Dr. Carlos Sunkel. In March of 1992 he joined back the Organic Chemistry Department of the University of Alcalá to work under the direction of Prof. Julio Alvarez-Builla in the group of Heterobetainas. In December of 1993 he carried out a second postdoctoral stay, with a NATO scholarship, under the direction of Prof. Steven M. Weinreb at Pennstate University, in Pennsylvania. In May of 1995 he return back to the Heterobetaínas group of the Organic Chemistry Department of the University of Alcalá. Since then he has been collaborating with Profs Alvarez-Builla and Juan José Vaquero. She initiated collaborations with Prof Sebastián Cerdán (Institute of Biomedical Research Alberto Sols, CSIC) and Prof Ernesto de Jesús (UD Inorganic Chemistry, UAH). In June 2001, she got a position as Lecturer of Organic Chemistry and in May of 2018 as Professor in the same field. She has been Vice Dean of the Faculty of Pharmacy in two periods: 1st Vice Dean (Nov 2002-January 2006) and 1st Vice Dean again (Feb 2009-May 2010). She is currently Director of the Dept. of Organic and Inorganic Chemistry of UAH (Jun 2016-). His topics of research include: Chemistry of Pyridinium N-Amines, Preparation and study of Calpain Inhibitors, Aceaminophen analogues and other topics related to Medicinal Chemistry and Synthetic Uses of Aryl and Heteroaryl Radicals.

Julio Alvarez-Builla Gómez was born in Madrid in 1946. He obtained his Doctorate in the Department of Organic Chemistry from the Faculty of Pharmacy of the Complutense University of Madrid, in 1976, working under the direction of Prof. G. Gonzalez Trigo. In 1978 he joined the group of Prof. A. R. Katritzky at the University of East Anglia (Norwich, UK). In 1980 he returned to the Complutense University, and in 1981 he joined the University of Alcalá, where he organized the Group of Heterobetaínas, a group that works in the field of heterocyclic chemistry, with an intense collaboration with pharmaceutical companies. In 1989 he organized, in collaboration with researchers from Organic Chemistry, Chemical Engineering, Analytical Chemistry and Microbiology, the Pilot Plant of Fine Chemicals, a research institute designed to develop University-Industry collaborations, from which he was appointed director in 1992 up to 2009. He has directed projects with Lilly, Glaxo SK, Janssen-Cilag, Servier, Cermol, Chemo (Geneve, Switzerland), IF Cantabria, St Charles Pharmaceuticals (N. Orleans, USA), and other companies in the chemical-pharmaceutical sector. In 1993 he obtained the chair of Organic Chemistry. From 1995 to 1998 he held the position of Vice-Rector for Research at the University of Alcalá. From 1998 to 2000, he was Vice Rector for Scientific and Technological Development, to promote University-Enterprise relations in the field of contract research activities. Prof. Alvarez-Builla is currently Emeritus Professor and keeps maintaining industrial projects and consulting activities.


Maria Luisa Izquierdo Ceinos completed her Degree in Chemical Sciences at the Complutense University of Madrid (UCM) (1974/1976). PhD in Sciences -Section Chemistry- by the UCM in 1983, with the presentation of the work "Synthesis of E- and Z-Cyclopropanecarboxylic Acids" conducted under the direction of Dr. D. M. Bernabé Pajares (CSIC). She did a Post-doctoral stay in the Chemistry Department of the Imperial College of Science and Technology (ICST) of London in the group of Prof. C.W. Rees, 1986. Her research work has been related to the synthesis, structural study and the reactivity of organic compounds included in the following areas: New Enzymatic Inhibitors - work of Degree and Doctoral Thesis, CSIC-, group Drs. E. Fernández-Álvarez and M. Bernabé. Chemistry of the Vinylazides -post-doctoral stage, ICST-, group Dr. C.W. Rees. Aza- and Diaza- Bi- and Triciclanos with Potential Pharmacological Activity -UAH-, group Prof. E. Gálvez. Azinium N-Heteroarylaminides -UAH-, group Prof. J. Alvarez-Builla. The work carried out is included in 44 scientific articles, 4 patents, the management of 7 Doctoral Theses and 49 congresses. Research activity has been recognized with four sexeniums. Teaching experience from 1975 to the present, has been developed in the UAH, recognized with six five-year terms. University Management for more than 15 years occupying statutory positions at departmental level: ViceDirector, Secretary and Director -7 years- of the Department of Organic Chemistry of the UAH. In July 2012 she received the Accreditation to University Professor.

Ramón Alajarín Ferrández Graduated in Chemistry at the Universidad Complutense and did his PhD in Chemistry at the University of Alcalá in 1993. He completed postdoctoral stays at the University of Exeter (United Kingdom, 1993) and at The Scripps Research Institute (California, USA, 1994-1995). Returning to Alcalá, he has been Assistant Professor (1996-2000) and Lecturer (2001-present) of the University of Alcalá. He develops his teaching and research activity in this University. Participates in the teaching of the Degrees of Chemistry and Pharmacy and in the Interuniversity Master of Discovery of Drugs. Research in the field of Organic Chemistry and Medical Chemistry. The current lines of research are: New synthetic methods; Inhibitors of therapeutic targets in Chronic Kidney Disease; Radiomarkers for the diagnosis of diseases related to neuroinflammation.


Elena Gala Sánchez began her Chemistry studies in 2008 at the University of Alcalá (UAH), obtaining the Degree in Chemistry in 2012 and the Master in Fine Chemistry in 2013. During this time, she joined the research group Heterobetaínas where she did the Work End of Degree, Final Master's and Doctorate under the supervision of Prof. Dr. Julio Álvarez-Builla and Dr. Mª Luisa Izquierdo, finally presenting her Doctoral Thesis in November 2018. In 2016 he completed his predoctoral stay in the group of Prof. Dr. Steven V. Ley at the University of Cambridge, working on the development of synthetic methodologies using Continuous Flow conditions.


Javier Recio Ramos began his Chemistry studies in 2009 at the University of Alcalá (UAH), obtaining the Degree in Chemistry in 2014 and the Master's Degree in Fine Chemistry in 2015, and developing the end-of-degree and master projects in the organic electrosynthesis group, under the tutoring of Dr. María Belén Batanero. In 2015 he joined the group of Heterobetaínas where he began his PhD studies under the supervision of Prof. Dr. Julio Álvarez-Builla and Prof. Dr. Carolina Burgos. In 2018 he made his predoctoral stay in the group of Prof. Dr. Axel Jacobi von Wangelin at the University of Hamburg, working on the development of new Luminol analogues and Sp3-Sp3 catalysts catalyzed by iron.


Publications

  • Gutierrez, M. Morón, M. Griera, D. Sucunza, L. Calleros, A. García-Jerez, C. Coderch, F. J. Hermoso, D. Rodriguez-Puyol, C. Burgos, M. Rodriguez-Puyol, B.Pascual-Teresa, M. L. Diaz-Marques, A. Jimenez, M. Toro-Londoño, J. Vaquero "DISCOVERY OF POTENT CALPAIN INHIBITORS BASED ON AZOLO-IMIDAZOLIDENONE SCAFOLD CORE" Eur. J. Med. Chem. 2018, 157, 946–959.
  • Malvicini, A. Gutierrez-Moraga, M.M. Rodriguez, S. Gomez-Bustillo, L. Salazar, C. Sunkel, L. Nozal, A. Salgado, M. Hidalgo, P. P. Lopez-Casas, et al “A TRICIN DERIVATIVE FROM DESCHAMPSIA ANTARCTICA DESV. INHIBITS COLORECTAL CARCINOMA GROWTH AND LIVER METASTASIS THROUGH THE INDUCTION OF A SPECIFIC IMMUNE RESPONSE” Molecular Cancer Therapeutics 2018, 17, 966-976.
  • Abet, F. Filace, J. Recio, J. Alvarez-Builla, C. Burgos "PRODRUG APPROACH: AN OVERVIEW OF RECENT CASES" Eur. J. Med. Chem. 2017, 127, 810–827.
  • Rodríguez-Sanz, P. Sánchez-Alonso, T. Bellón, R. Alajarin, V. Martínez-Cabeza, R. Selgas, J.J Vaquero, J. Álvarez-Builla “SYNTHESIS AND BIOLOGICAL EVALUATION OF PYRIDAZINO[1',6':1,2]PYRIDO[3,4-B]INDOLINIUM AND PYRIDAZINO[1,6-A]BENZIMIDAZOLIUM SALTS AS ANTI-INFLAMMATORY AGENTS” Eur. J. Med. Chem. 2015, 93, 83–92.
  • Nieto, M. Delgado, M. Sobrado, M. De Ceballos, R. Alajarin, L. Garcia-Garcia, J. Kelly, I. Lizasoain, M. Pozo, J. Alvarez-Builla ”PRELIMINARY RESEARCH ON 1-(4-BROMO-2-NITROIMIDAZOL-1-YL)-3-[18F]FLUOROPROPAN-2-OL AS A NOVEL BRAIN HYPOXIA PET TRACER IN A RODENT MODEL OF STROKE” Eur. J. Med. Chem. 2015 101, 604-615.
  • García, V. Abet, R. Alajarín, J. Álvarez-Builla, M. Delgado, L. García-García, P. Bascuñana-Almarcha, C. Peña-Salcedo, J. Kelly, M. A. Pozo “N-(4-[18F]-FLUORO-2-PYRIDINYL)-N-[2-[4-(2-METHOXYPHENYL)-1-PIPERAZINYL] ETHYL] CARBOXAMIDES AS ANALOGS OF WAY100635. NEW PET TRACERS OF SEROTONIN 5-HT1A RECEPTORS “ Eur. J. Med. Chem. 2014, 85, 795–806.
  • A. I. Sanchez, R. Meneses, J. M. Minguez, A. Nunez, R. R. Castillo, F.  Filace, C. Burgos, J. J. Vaquero, J. Alvarez-Builla, A. Cortes-Cabrera, F. Gago, E. Terricabras, V. Segarra "MICROWAVE-ASSISTED SYNTHESIS OF POTENT PDE7 INHIBITORS CONTAINING A THIENOPYRIMIDIN-4-AMINE SCAFFOLD" Org. Biomol. Chem.  2014, 12, 4233–4242.

The following patents are also indicated: ES 2457671 A1 20140428 (2014), ES 2522717 A1 20141117 (2014), PCT Int. Appl. WO 2015004304 A1 20150115 (2015), ES 2537221 A1 20150603 (2015), ES 2526935 A1 20150116 (2015), ES 2529865 A1 20150225 (2015). , PCT Int. Appl. WO 2015011331 A1 20150129 (2015), PCT Int. Appl. (2016), WO 2016144995 A1 20160915, U.S. Pat. Appl. Publ. (2017), US 20170049839 A1 20170223., Application Number:62550137 PCT/US2018/22029

Contact

Carolina Burgos García - carolina.burgos@uah.es


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