Source: http://doczz.es/doc/25242/diapositiva-1
Timestamp: 2019-04-19 09:12:24+00:00

Document:
Biological Chemistry 279 (30), 31429-31439.
Edition, Editor(s): William P. Janzen, Paul Bernasconi (Springer), pp. 69-106.
Laura Vela, Peter N. Lowe, John Gerstenmaier, Lance G. Laing, Julie B. Stimmel, Lisa A.
emerged as the pharmaceutical industry´s grand challenge.
R&D productivity. Seeking and finding the golden needles in the haystack seemed feasible.
chemical space and decrease the attrition towards drug candidate selection?
Autónoma University for his work on the field of CCKA antagonists.
also member of the Spanish Medicinal Chemistry Society.
preclinical models of positive, cognitive and negative symptoms.
optimized PDE10A inhibitor 23 will be described.
Tandon, R.; Nasrallah, H.A.; Keshavan, M.S. Schizophr. Res. 2009, 110, 1–23.
Conn, J. P.; Lindsley, C. W.; Jones, C. K. Trends Pharmacol Sci. 2009, 30, 148-155.
Macdonald, G.J.; Bartolome J.M. Progress in Medicinal Chemistry 2010, 49, 37-80.
– Risperidone, Paliperidone Olanzapine, Aripiprazole, Quetiapine….
non-cyclic AMP to the beads.
– Autoradiographic characterization of [3H]ref.
– No potential to induce CYP3A4 and 1A2.
Post doc at Imperial College, London, U.K.
 A Degree not just in chemistry, but with many hours of biology, physics and rock guitar.
collaborations. Here, I learnt to work.
systems and a new language. I am still learning.
Senior Scientist, Medicinal Chemistry Department. Almirall S.A.
The measurement of ligand binding potency is fundamental to Medicinal Chemistry.
finishing with a case study from a recent research program.
Medicinal Chemistry in a nutshell ….
RO: How far does the seesaw tip?
Biotech 1 has identified an over-active enzyme ENZ1 which converts PIM into potentially harmful PAM.
You want to identify inhibitors of this enzyme ENZ1.
which is necessary for good health.
You want to identify selective blockers of SIG1.
suffer from an embarrassing problem.
 Choose 3 of the strategies listed and think how they might apply to your project.
 Each Biotech will select a CEO to present their case to the Venture Capitalist.
 Explain your choice of the 3 strategies and why you think these will be useful to your project.
GlaxoWellcome in Madrid as a graduate trainee, working a protein kinase C project.
P. falciparum DHODH targets as well as phenotypic approaches.
with other institutions in the discovery of novel antikinetoplastida drugs.
preparation of technical and regulatory documents, and interacting with regulatory agencies.
likelihood that a toxic effect can be produced at an expected exposure level and condition).
of drug substance related impurities can be taken into account.
impurities in pharmaceuticals that possess potential for genotoxicity. Regulatory Tox.
(Snodin DJ (2010). Genotoxic Impurities: From Structural Alerts to Qualification.
PhD (Chemistry, Universidad de Oviedo).
Participation at numerous postgraduate programs.
presented many oral and poster communication in congresses.
Section Chief, Synthesis Department, Faes Farma S.A.
synthetic routes using low-cost raw materials with a minimal waste output, suitable for scaleup.
Víctor Rubio, Faes Farma S.A.
Anyy action to minimize them?
Any action to minimize it?
How to make a process less expensive ???
2-Add ethyldiisopropylamine and cumene hydroperoxide, at 30ºC.
Priscila G. Alves Martins , Ruben Gonzalez del Rio , Pedro A. Torres-Gomez , Eva M.
evaluation of activity and toxicity of those inhibitors in in vitro assays is the main objective of this work.
in activated macrophages infected with Mycobacterium bovis BCG are in progress.
http://apps.who.int/iris/bitstream/10665/75938/1/9789241564502_eng.pdf (acessed April 28 2013).
Zhang, Z. Y. Targeting mycobacterium protein tyrosine phosphatise B for antituberculosis agents. Proc. Natl. Acad. Sci. U.S.A.
inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatases (PtpA and PtpB). Journal of Medicinal Chemistry.
with control of cancer processes.
galactose have been attached to pyridostatin aromatic derivatives .
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Beatriz Balsera, Mª Ángeles Bonache, Mª Jesús Pérez de Vega and Rosario González Muñiz.
Instituto de Química Médica, Juan de la Cierva 3, 28006-Madrid.
able to modulate some TRP channels.
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Santiago de Compostela, c/ Jenaro de la Fuente s/n, 15782 Santiago de Compostela, Spain.
the third enzyme of the pathway, the dehydroquinase enzyme (DHQ2), which is essential in H. pylori.
improved activity. In this communication, we will present our latest results in this project.
the Spanish Ministry of Science and Innovation for their respective FPU fellowships.
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5. Peón, A.; Coderch, C.; Gago, F.; González-Bello, C. ChemMedChem 2013, DOI:10.1002/cmdc.201300013.
1Drug Discovery Platform (PDD), Parc Cientific de Barcelona, Barcelona, Spain.
Research Institute - Universitat Pompeu Fabra, Barcelona, Spain.
Universidad de Santiago de Compostela (USC), Santiago de Compostela, Spain.
which experimental validation of new biological targets was determined.
of an effective and safe therapy of BPSD remains an increasing clinical and social unmet need.
Moreover recent clinical findings confirm their utility in treatment of Alzheimer’s disease .
antagonists with aryloxy fragments providing D2 partial agonism .
novel indoleamine-based hybrid molecules indicates their relevance for BPSD drug discovery.
derivatives for the treatment of CNS disorders’ WO 2013/001499.
Farmaco Chimico e Tecnologico, Università degli Studi di Siena, via Alcide de Gasperi 2, 53100 Siena, Italy.
cases (MDR-TB) is continuously increasing, thus a new shorter and simpler drug regimens is needed.
four hit compounds (BM212, BM521, BM533, BM579) was evaluated for drug-like properties.
potent and selective agents against neoplastic cells.
structural diversity involving the different ring positions (N2, C4, C5 and C6).
no previous data in literature about hybrid compounds pyridazinone dithiocarbamate.
from one to three carbons has been designed as potential anticancer agents (Figure 1).
amines and CS2 in the presence of K3PO4 provided the new hybrid analogues in good yield.
values in the M range. The results of this study will be discussed.
We acknowledge the Xunta de Galicia and the Universidade de Vigo for the financial support.
H. Frank, G. Heinisch, Ibid 1992, 141-183.
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VPg to act as the primer for both positive- and negative-strand synthesis.
thus, blocking the access of the template and of the incoming nucleotides.
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Mario de la Fuente Revenga , Anders A. Jensen , Thomas Balle and Bente Frølund .
selective ligands in order to exploit the small differences present in the receptor cavity.
in the pharmaceutical market, exist a large number of structures carrying nitrogenous substances.
activity on different therapeutic targets.
therapeutic target for the control of this disease.
the active site and the inhibitor and it is an additional aid to organic synthesis for drug design.
Kouznetsov, V. Tetrahedron. 2009, 65, 2721–2750.
Maccioni, R.B.; Barbeito, L.; Muñoz, J.P.; Arch. Med. Res. 2001, 32, 367-381.
compounds incorporating the coumarin moiety with remarkable activity towards MAO and/or AChE.
studies and further completion of the substituted series are currently in progress.
Figure 1 – 3,6-disubsituted coumarins series.
the Treatment of Alzheimer’s Disease”, Med Chem Commun, 3, (2012), 213–218.
Fatty acid synthase (FASN) is overexpressed in human breast carcinoma and other human cancers.
number and position of the hydroxy groups (R1-R3).
determined for UCM028 indicate a higher metabolic stability than that of natural inhibitor EGCG.
Ortega-Gutiérrez, S.; Relat, J.; Oliveras, G.; Blancafort, A.; Haro, D.; Marrero, P. F.; Colomer, R.; López-Rodríguez, M. L. J.
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obtain pyrazines 10, quinazolines 11 and imidazole derivatives 12.
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Farmacología, Universidad Complutense de Madrid.
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To develop the series into compounds with lead-like properties for anti-Malarial agents.
novel serine protease targets in Plasmodia.
compounds have displayed interesting properties. Current work is focussing on development of this series.
in vitro suitable for target identification.
NEUROPROTECTIVE AGENTS ACTING AS SIGMA1 RECEPTOR AGONISTS.
ISOLATION, CONFIGURATIONAL ASSIGNMENT AND BIOLOGICAL PROFILE.
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Department de Ciències Experimentals i de la Salut. Universitat Pompeu Fabra, Barcelona,Spain.
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Department of Pharmacology, Faculty of Pharmacy, University of Santiago de Compostela, Spain.
Deparment of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, Spain.
interesting vasorelaxant activity and platelet aggregation inhibition for these new derivatives.
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Norbert Klotz3, Stefano Moro4, Stefano Alcaro5, Fernanda Borges1.
Francisco J. Ortega 1, Mar Martín-Fontecha 1, Moisés Balabasquer 1, Ian Cushman 2, Iván R.
Investigaciones Biológicas, Consejo Superior de Investigaciones Científicas, Madrid E-28040, Spain.
approach to anticancer drug development.
show good pharmacokinetic properties.4 All these results and the ongoing research will be presented.
Economía y Competitividad (MINECO, SAF2010-22198) and Comunidad de Madrid (SAL2010/MBD2353). The authors thank MINECO for predoctoral FPI fellowships to M.B. and F.J.O.
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Instituto de Química Médica (IQM-CSIC), Madrid, España.
Universidad de Alcalá. Alcalá de Henares, España.
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Pharmacotherapy Lab., Instituto de Salud Tropical, CIMA, Avda. Pío XII, 55, 31008 Pamplona.
compound 1c is the most active and currently in the second stage of in vitro evaluation.
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CIQUP/Department of Chemistry and Biochemistry - Faculty of Sciences of Porto, Porto - Portugal.
Organic Chemistry Department, Faculty oh Pharmacy, University of Santiago de Compostela, Spain.
Department of Pharmacology and Toxicology, University of Würzburg, Germany.
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restrictions related with side effects, low absorption, short-half-life and toxicity .
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(SFRH/BD/61262/2009) and F. Borges (SFRH/BSAB/1090/2010) thank FCT grants.
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properties of novel compounds with donepezil.
Vigo for a pre-doctoral contract.
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(MINECO, SAF2010-22198) and Comunidad de Madrid (S2010/BMD-2353). The author thanks MINECO for predoctoral F.P.U.
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HYBRIDS, A NOVEL CLASS OF ANTIMALARIALS.
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Figure 1: Tetraoxane – pyrimidine nitrile hybrids.
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In 2010 there were about 219 million cases of malaria and near 660000 people died .
hypnozoites. However, primaquine exhibit a poor activity against blood-stage of malaria parasite .
the malaria parasite. The synthesis and activity of the synthesized compounds will be presented.
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presenting a peptide-like backbone conjugated to nucleobases through different linker moieties.
with high affinity while still displaying sufficient specificity to distinguish single-base mismatches.
Scheme 1: Nucleobase-functionalized cysteines and cysteinyl dipeptide.
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is also acknowledged for the PhD grant SFRH/BD/61611/2009.
specific stage of the parasite’s life cycle, in a single molecule called hybrid drug.
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were designed, tested and crystallized with the enzyme. Our progress in the project will be presented.
and designed substrate analogs 35.
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biological activity are also provided.
binding mode of the most active compound in the enzyme active site.
Spanish Ministry of Science and Innovation for his FPI fellowship.
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bacteria, such as M. tuberculosis, H. pylori, A. baylyi, H. influenzae, F. novicida and P. aeruginosa.
available. In this communication, our latest results in the project will be presented.
section of the active site of the SK enzyme from M. tuberculosis.
Spanish Ministry of Science and Innovation for her FPI fellowship.
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Noetzel 3,4, Emily Days 3,7, C. David Weaver 3,7, Craig W. Lindsley 3,4,5,6, Colleen M.
Development, Jarama 75, 45007-Toledo, Spain.
University Medical Center, Nashville, TN 37232, USA.
Vanderbilt Specialized Chemistry Center for Probe Development (MLPCN), Nashville, TN 37232, USA.
Janssen Research and Development, Turnhoutseweg 30, B-2340, Beerse, Belgium.
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