133003-98-2Relevant academic research and scientific papers
N,N'-Di(8-quinolyl)glutaramide Exhibiting Highly Selective and Efficient Uphill Transport of Cu(II) through Liquid Membranes
Hiratani, Kazuhisa,Kasuga, Kazuyuki,Hirose, Takuji,Taguchi, Kazuhiro,Fujiwara, Kyoko
, p. 2381 - 2387 (1992)
N,N'-Di(8-quinolyl)glutaramide has been found to be an excellent Cu(II) carrier in the transport through a chloroform liquid membrane.It can selectively and efficiently transport Cu(II) from a weakly acidic aqueous solution containing Cu(II), Zn(II), Ni(II), and Co(II).Several N,N'di(8-quinolyl)glutaramide derivatives and their analogues have been prepared for comparison of this transport ability, which largely depends not only upon te structure of the carriers, but also upon the transport conditions.
Synthesis and binding assays of novel 3,3-dimethylpiperidine derivatives with various lipophilicities as σ1 receptor ligands
Ferorelli, Savina,Abate, Carmen,Pedone, Maria P.,Colabufo, Nicola A.,Contino, Marialessandra,Perrone, Roberto,Berardi, Francesco
experimental part, p. 7612 - 7622 (2012/01/04)
Starting from two carbocyclic analogs, a series of 3,3-dimethylpiperidine derivatives was prepared and tested in radioligand binding assays at σ1 and σ2 receptors, and at Δ8-Δ7 sterol isomerase (SI) site. The novel compounds mostly bear heterocyclic rings or bicyclic nucleus of differing lipophilicities. Compounds 18a and 19a,b demonstrated the highest σ1 affinity (Ki = 0.14-0.38 nM) with a good selectivity versus σ2 binding. Among them, 18a had the lowest C log D value (3.01) and only 19b was selective versus SI too. Generally, it was observed that more planar and hydrophilic heteronuclei conferred a decrease in affinity for both σ receptor subtypes.
7-azaindol-3-ylacrylamides active as kinase inhibitors
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Page/Page column 87-88, (2009/07/10)
Compounds represented by Formula (I) wherein R1 and R2 are as defined in the specification, compositions thereof, and methods of use thereof.
A multireceptorial binding reinvestigation on an extended class of σ ligands: N-[ω-(indan-1-yl and tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine reveal high affinities towards σ1 and EBP sites
Berardi, Francesco,Ferorelli, Savina,Colabufo, Nicola Antonio,Leopoldo, Marcello,Perrone, Roberto,Tortorella, Vincenzo
, p. 1325 - 1335 (2007/10/03)
New 1-[ω-(2,3-dihydro-1H-inden-1-yl)- and (2,3-dihydro-5-methoxy-1H-inden-1-yl)alkyl]- and 1-[ω-(1,2,3,4-tetrahydronaphthalen-1-yl)- and (6-methoxy- or 6-fluoro-1,2,3,4-tetrahydronaphthalen-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine were synthesized, as homologous compounds of an existing series of σ ligands, in order to carry out σ receptor subtypes structure-affinity relationships. The new compounds and some of their related analogues, already reported, were tested in new multireceptorial radioligand binding assays. As reference compounds, the known σ1 ligands SA 4503, BD 1008 and NE 100 were also prepared and tested. All reported compounds showed high σ1 affinity assayed by (+)-[3H]-pentazocine on guinea-pig brain (apparent Ki=1.75-72.2 nM) and moderate or low σ2 affinity by [3H]-DTG on rat liver, in contrast with previous results. One tertiary amine function spaced by a five-membered chain from a phenyl group is the structural feature shared by the most active compounds 26 and 43 and some reference σ1 ligands. The reported σ1 ligands, including reference compounds, also demonstrated a high affinity towards EBP (Δ8-Δ7 sterol isomerase) site (apparent Ki=0.48-14.8 nM) and some of them (37 and 44) were good ligands at L-type Ca++ channel. 1-[4-(2,3-Dihydro-1H-inden-1-yl)butyl]-3,3-dimethylpiperidine (26) was the best mixed σ1 and EBP ligand (apparent Ki=1.75 and 1.54 nM, respectively) with a good selectivity versus σ2 receptor (138- and 157-fold, respectively).
