267242-64-8Relevant articles and documents
Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2
Lucas, Rut,Ubeda, Amalia,Paya, Miguel,Alves, Mario,Olmo, Esther Del,Lopez, Jose L.,San Feliciano, Arturo
, p. 285 - 288 (2000)
We have synthesised some lipidic diamines and aminoalcohols and examined their behaviour as inhibitors of secretory and cytosolic PLA2. Some structure-activity relationships considerations have been deduced. Compound 14 was a potent and selective inhibitor of cPLA2 and compound 4 showed a dual inhibitory profile against both types of PLA2 while no cytotoxicity at 10 μM on human neutrophils or on murine macrophage line was observed for both. (C) 2000 Elsevier Science Ltd. All rights reserved.
Synthesis and evaluation of some lipidic aminoalcohols and diamines as immunomodulators
Olmo, Esther del,Plaza, Alvaro,Muro, Antonio,Martinez-Fernandez, Antonio R.,Nogal-Ruiz, Juan J.,Lopez-Perez, Jose L.,Feliciano, Arturo San
, p. 6091 - 6095 (2007/10/03)
Lymphoproliferation inhibition and cytotoxicity of a number of lipidic aminoacids, aminoalcohols and diamines were evaluated as a preliminary screening to select potential immunomodulators. The four most potent/less toxic compounds were submitted to delayed hypersensibility (DTH) assays to define the best to be evaluated further Graft-vs-Host, NO production and other immunoevaluation (CD4+, CD45, CD8, CD11b, I-Ek, and NK cells) assays, to establish their immunomodulation potential for being further considered as auxiliary agents for vaccination against some parasitic infections. Compounds 5d, 6d, 6f, 7a, and 9a, fairly inhibited the lymphoproliferation (71.6-79.5%, at 3.2-2.4 nM), while the aminoalcohol derivative 6f and the diamine 7a gave the most promising results in the DTH assays. Diamine derivative 8b induced nitrite production on normal macrophages, whereas compounds 6f and 7a induced nitrite production on LPS pre-stimulated macrophages. These two last compounds have been selected to follow in vivo vaccination assays.
Long-chain aminoalcohol and diamine derivatives induce apoptosis through a caspase-3 dependent pathway
Del Olmo, Esther,Macho, Antonio,Alves, Mario,Lopez, Jose L.,Banoua, Fadwa,Muoz, Eduardo,San Feliciano, Arturo
, p. 2621 - 2626 (2007/10/03)
A number of long chain diamines and aminoalcohols and several of their alkyl, acyl and carbamoyl derivatives, have been synthesized and evaluated for their apoptotic activities using the Jurkat cell line. Apoptosis was measured by flow cytometry and the best results were found for the aminoalcohols displaying either a free alcohol or an amine with at least, one free hydrogen atom. The apoptotic pathway was mediated by a disruption of the mitochondria transmembrane potential and caspase-3 activation, inducing DNA fragmentation at the phase G1/S of the cell cycle.
