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Synthesis and evaluation of compounds potentially ligands of H4 receptors

Grant number: 13/20479-9
Support type:Regular Research Grants
Duration: April 01, 2014 - July 31, 2016
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:João Paulo dos Santos Fernandes
Grantee:João Paulo dos Santos Fernandes
Home Institution: Instituto de Ciências Ambientais, Químicas e Farmacêuticas (ICAQF). Universidade Federal de São Paulo (UNIFESP). Campus Diadema. Diadema , SP, Brazil
Assoc. researchers:Lanfranco Ranieri Paolo Troncone


Histamine is a chemical transmitter found practically in whole organism, and exerts its effects through the interaction with H1 to H4 histaminergic receptors. Specifically, H4 receptors are found mainly in immune cells and blood-forming tissues, thus are involved in inflammatory and immune processes, as well as some actions in CNS. Therefore, H4 receptor ligands can have applications in the treatment of chronic inflammatory and immune diseases, and may be a novel therapeutic option in these conditions. However, despite the high homology between H3 and H4 receptors, these ligands should present adequate selectivity to avoid side effects. This project aims to perform synthesis of substituted 2,3-dihydrobenzofuryl- and 2,3-dihydroindolyl-methylpiperazines and to evaluate its binding activity in H3 and H4 receptors, in order to define the structural features that determine the affinity and selectivity to H4 receptor. The project is a continuation of developed works by the author, and thereby, some synthetic methodologies are already defined and published, but the final compounds still are unpublished and patentable. It is expected the compounds exhibit good H4 affinity and selectivity, and the results could evidence the relationship between structure and activity of the compounds, to help the future design of more active and selective compounds. (AU)

Scientific publications (7)
(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)
CORREA, MICHELLE F.; BARBOSA, ALEFE J. R.; TEIXEIRA, LARISSA B.; DUARTE, DIEGO A.; SIMOES, SARAH C.; PARREIRAS-E-SILVA, LUCAS T.; BALBINO, ALEKSANDRO M.; LANDGRAF, RICHARDT G.; BOUVIER, MICHEL; COSTA-NETO, CLAUDIO M.; FERNANDES, JOAO P. S. Pharmacological Characterization of 5-Substituted 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazines: Novel Antagonists for the Histamine H-3 and H-4 Receptors with Anti-inflammatory Potential. FRONTIERS IN PHARMACOLOGY, v. 8, NOV 14 2017. Web of Science Citations: 7.
OLIVEIRA, DANIELA R.; LUCHEZ, CIBELE V.; BORTOLOTTO, ZUNER A.; FERNANDES, JOAO P. S. Evaluation of -Aminocarboxylic Acid Derivatives in Hippocampal Excitatory Synaptic Transmission. ARCHIV DER PHARMAZIE, v. 350, n. 11 NOV 2017. Web of Science Citations: 0.
CORREA, MICHELLE FIDELIS; VARELA, MARINA THEMOTEO; BALBINO, ALEKSANDRO MARTINS; TORRECILHAS, ANA CLAUDIA; LANDGRAF, RICHARDT GAMA; PAOLO TRONCONE, LANFRANCO RANIERI; DOS SANTOS FERNANDES, JOAO PAULO. 1-[(2,3-Dihydro-1-benzofuran-2-yl) methyl]piperazines as novel anti-inflammatory compounds: Synthesis and evaluation on H3R/H4R. CHEMICAL BIOLOGY & DRUG DESIGN, v. 90, n. 2, p. 317-322, AUG 2017. Web of Science Citations: 6.
SANTOS NASCIMENTO, LILLIAN FERREIRA; SANTOS FERNANDES, JOAO PAULO. Factorial study to assess an ultrasonic methodology for the allylation of 4-chloroaniline. GREEN PROCESSING AND SYNTHESIS, v. 6, n. 2, p. 203-209, APR 2017. Web of Science Citations: 0.
SEGRETTI, NATANAEL DANTE; SIMOES, CRISTINA KORTSTEE; CORREA, MICHELLE FIDELIS; ANDRES FELLI, VENI MARIA; MIYATA, MARCELO; CHO, SANG HYUN; FRANZBLAU, SCOTT GARY; DOS SANTOS FERNANDES, JOAO PAULO. Antimycobacterial activity of pyrazinoate prodrugs in replicating and non-replicating Mycobacterium tuberculosis. TUBERCULOSIS, v. 99, p. 11-16, JUL 2016. Web of Science Citations: 4.
CORREA, MICHELLE FIDELIS; RAMOS BARBOSA, ALEFE JHONATAS; SATO, RIE; JUNQUEIRA, LUIS OTAVIO; POLITI, MARIO JOSE; RANDO, DANIELA GONCALES; DOS SANTOS FERNANDES, JOAO PAULO. Factorial design study to access the ``green{''} iodocyclization reaction of 2-allylphenols. GREEN PROCESSING AND SYNTHESIS, v. 5, n. 2, p. 145-151, APR 2016. Web of Science Citations: 4.
VARELA, MARINA T.; DIAS, ROBERTO Z.; MARTINS, LIGIA F.; FERREIRA, DAIANE D.; TEMPONE, ANDRE G.; UENO, ANDERSON K.; LAGO, JOAO HENRIQUE G.; FERNANDES, JOAO PAULO S. Gibbilimbol analogues as antiparasitic agents-Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum. Bioorganic & Medicinal Chemistry Letters, v. 26, n. 4, p. 1180-1183, FEB 15 2016. Web of Science Citations: 8.

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