119754-18-6Relevant articles and documents
Metal Complex Lipids for Fluid–Fluid Phase Separation in Coassembled Phospholipid Membranes
Anegawa, Yuka,Hayami, Shinya,Kato, Koichi,Kawano, Kenichi,Kinoshita, Masanao,Matsumori, Nobuaki,Nakamura, Masaaki,Ohba, Masaaki,Ohtani, Ryo,Tajima, Yutaro,Watanabe, Hikaru,Yanaka, Saeko
supporting information, p. 13603 - 13608 (2021/05/10)
We demonstrate a fluid–fluid phase separation in 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) membranes using a metal complex lipid of type [Mn(L1)] (1; HL1=1-(2-hydroxybenzamide)-2-(2-hydroxy-3-formyl-5-hexadecyloxybenzylideneamino)ethane). Small a
Selectivity Optimization of Substituted 1,2,3-Triazoles as α7 Nicotinic Acetylcholine Receptor Agonists
Arunrungvichian, Kuntarat,Fokin, Valery V.,Vajragupta, Opa,Taylor, Palmer
, p. 1317 - 1330 (2015/09/01)
Three series of substituted anti-1,2,3-triazoles (IND, PPRD, and QND), synthesized by cycloaddition from azide and alkyne building blocks, were designed to enhance selectivity and potency profiles of a lead α7 nicotinic acetylcholine receptor (α7-nAChR) agonist, TTIn-1. Designed compounds were synthesized and screened for affinity by a radioligand binding assay. Their functional characterization as agonists and antagonists was performed by fluorescence resonance energy transfer assay using cell lines expressing transfected cDNAs, α7-nAChRs, α4β2-nAChRs, and 5HT3A receptors, and a fluorescence cell reporter. In the IND series, a tropane ring of TTIn-1, substituted at N1, was replaced by mono- and bicyclic amines to vary length and conformational flexibility of a carbon linker between nitrogen atom and N1 of the triazole. Compounds with a two-carbon atom linker optimized binding with Kds at the submicromolar level. Further modification at the hydrophobic indole of TTIn-1 was made in PPRD and QND series by fixing the amine center with the highest affinity building blocks in the IND series. Compounds from IND and PPRD series are selective as agonists for the α7-nAChRs over α4β2-nAChRs and 5HT3A receptors. Lead compounds in the three series have EC50s between 28 and 260 nM. Based on the EC50, affinity, and selectivity determined from the binding and cellular responses, two of the leads have been advanced to behavioral studies described in the companion article (DOI: 10.1021/acschemneuro.5b00059).
Compounds containing an amino salicylic acid moiety linked to a sulphapyridine moiety via stable bridge
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, (2008/06/13)
A compound of the formula Het--NR--SO2 --Ph2 --A--Ph1 (COOH)(OH) and tautomeric form, salts, solvates, C1-6 alkyl esters and pharmaceutical compositions of the compound. Ph1 and Ph2 are ben