In an article, author is Corre, Michelle F., once mentioned the application of 497-23-4, Recommanded Product: Furan-2(5H)-one, Name is Furan-2(5H)-one, molecular formula is C4H4O2, molecular weight is 84.07, MDL number is MFCD00005376, category is benzofurans. Now introduce a scientific discovery about this category.
Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands – Functional characterization and modeling studies on H-3 and H(4 )receptors
Histamine acts through four different receptors (H1R-H4R), the H3R and H4R being the most explored in the last years as drug targets. The H3R is a potential target to treat narcolepsy, Parkinson’s disease, epilepsy, schizophrenia and several other CNS-related conditions, while H4R blockade leads to anti-inflammatory and immunomodulatory effects. Our group has been exploring the dihydrobenzofuranyl-piperazines (LINS01 series) as human H3R/H4R ligands as potential drug candidates. In the present study, a set of 12 compounds were synthesized from adequate (dihydro)benzofuran synthons through simple reactions with corresponding piperazines, giving moderate to high yields. Four compounds (1b, 1f, 1g and 1h) showed high hH(3)R affinity (pK(i) > 7), compound 1h being the most potent (pK(i) 8.4), and compound if showed the best efficiency (pKi 8.2, LE 0.53, LLE 5.85). BRET-based assays monitoring G alpha(i) activity indicated that the compounds are potent antagonists. Only one compound (2c, pK(i) 7.1) presented high affinity for hH(4)R. In contrast to what was observed for hH(3)R, it showed partial agonist activity. Docking experiments indicated that bulky substituents occupy a hydrophobic pocket in hH(3)R, while the N-allyl group forms favorable interactions with hydrophobic residues in the TM2, 3 and 7, increasing the selectivity towards hH(3)R. Additionally, the importance of the indole NH in the interaction with Glu5.46 from hH(4)R was confirmed by the modeling results, explaining the affinity and agonistic activity of compound 2c. The data reported in this work represent important findings for the rational design of future compounds for hH(3)R and hH(4)R.
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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem