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Synthesis, chemical and biological characterization of 2-phenyl quinazolines-4-substituted analogues as novel atypical dopamine transporter (ADT) and reuptake inhibitors

Grant number: 16/10149-0
Support Opportunities:Scholarships abroad - Research
Effective date (Start): March 10, 2017
Effective date (End): March 09, 2018
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Organic Chemistry
Principal Investigator:Eduardo Rene Perez Gonzalez
Grantee:Eduardo Rene Perez Gonzalez
Host Investigator: Gert Lubec
Host Institution: Faculdade de Ciências e Tecnologia (FCT). Universidade Estadual Paulista (UNESP). Campus de Presidente Prudente. Presidente Prudente , SP, Brazil
Research place: University of Vienna, Austria  


Dopamine (DA) was identified as a neurotransmitter in the brain, about 50 years ago and has been the subject of an extraordinary number of researches and publications. Due to the early discovery of a strong correlation between the depletion of the DA striatal and motor deficits observed in Parkinson's disease (PD), the involvement in the motion control has long been emphasized. The discovery of the role in the motor components of the DA began a long series of experiments and clinical investigations, which are still in progress, leading to the development of L- DOPA therapy and, later, for other types of medications to improve the patient's symptoms. The Theme proposed for the postdoc offers the possibility of synthesizing heterocyclic systems that have activity against neurodegenerative diseases, Alzheimer's type, in the treatment of schizophrenia and autism, as well as to the improvement of the cognitive process and also as antitumor. This class of molecules could find use in the treatment of alcoholism and addiction of cocaine and amphetamines. Possible concomitant mechanism of inhibition of Kv3.1 potassium ion channels will be investigated for the sulfonamide-quinazoline and sulfonamide-fluoxetine derivatives, synthesized during the present research. The compounds synthesized in this work will be fully characterized by spectroscopic and spectrometric analysis and studied for their biological properties in vitro and in vivo using the methods described. (AU)

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Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
KALABA, PREDRAG; AHER, NILIMA Y.; ILIC, MARIJA; DRAGACEVIC, VLADIMIR; WIEDER, MARCUS; MIKLOSI, ANDRAS G.; ZEHL, MARTIN; WACKERLIG, JUDITH; ROLLER, ALEXANDER; BERYOZKINA, TETYANA; et al. Heterocyclic Analogues of Modafinil as Novel, Atypical Dopamine Transporter Inhibitors. Journal of Medicinal Chemistry, v. 60, n. 22, p. 9330-9348, . (16/10149-0)
KALABA, PREDRAG; ILIC, MARIJA; AHER, NILIMA Y.; DRAGACEVIC, VLADIMIR; WIEDER, MARCUS; ZEHL, MARTIN; WACKERLIG, JUDITH; BEYL, STANISLAV; SARTORI, SIMONE B.; EBNER, KARL; et al. Structure-Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters. Journal of Medicinal Chemistry, v. 63, n. 1, p. 391-417, . (16/10149-0)
DA SILVA, SUZANE ROSA; KALABA, PREDRAG; FABISIKOVA, ANNA; ZEHL, MARTIN; DRAGATEVIE, VLADIMIR; DOS ANJOS, LUANA RIBEIRO; NEILL, PHILIP JOHN; WIEDER, MARCUS; PRADO-ROLLER, ALEXANDER; GAJIC, NATALIE; et al. ynthesis and dopamine receptor binding of dihydrexidine and SKF 38393 catecholamine-based analogue. Amino Acids, v. 54, n. 1, . (16/10149-0, 18/00581-7)

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