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Title: 1-[(2,3-Dihydro-1-benzofuran-2-yl) methyl]piperazines as novel anti-inflammatory compounds: Synthesis and evaluation on H3R/H4R
Authors: Correa, Michelle Fidelis [UNIFESP]
Varela, Marina Themoteo [UNIFESP]
Balbino, Aleksandro Martins [UNIFESP]
Torrecilhas, Ana Claudia [UNIFESP]
Landgraf, Richardt Gama [UNIFESP]
Paolo Troncone, Lanfranco Ranieri
dos Santos Fernandes, Joao Paulo [UNIFESP]
Keywords: anti-inflammatory agent
H3R ligand
H4R ligand
histamine receptor
Issue Date: 2017
Publisher: Wiley
Citation: Chemical Biology & Drug Design. Hoboken, v. 90, n. 2, p. 317-322, 2017.
Abstract: The histamine receptors (HRs) are members of G-protein-coupled receptor superfamily and traditional targets of huge therapeutic interests. Recently, H3R and H4R have been explored as targets for drug discovery, including in the search for dual-acting H3R/H4R ligands. The H4R, the most recent histamine receptor, is a promising target for novel anti-inflammatory agents in several conditions such as asthma and other chronic inflammatory diseases. Due to similarity with previously reported ligands of HRs, a set of 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazines were synthesized and evaluated in competitive binding assays as H3R/H4R ligands herein. The results showed the compounds presented affinity (K-i) for H3R/H4R in micromolar range, and they are more selective to H3R. All the compounds showed no important cytotoxicity to mammalian cells. The phenyl-substituted compound LINS01005 has shown the higher affinity of the set for H4R, but no considerable selectivity toward this receptor over H3R. LINS01005 showed interesting anti-inflammatory activity in murine asthma model, reducing the eosinophil counts in bronchoalveolar lavage fluid, as well as the COX-2 expression. The presented compounds are valuable prototypes for further improvements to achieve better anti-inflammatory agents.
ISSN: 1747-0277
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