267242-65-9Relevant articles and documents
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis
del Olmo, Esther,Molina-Salinas, Gloria Maria,Escarcena, Ricardo,Alves, Mario,Lopez-Perez, Jose L.,Hernandez-Pando, Rogelio,Said-Fernandez, Salvador,Feliciano, Arturo San
scheme or table, p. 5764 - 5768 (2010/04/05)
Fifteen dihydrosphingosine analogues have been synthesized and tested in vitro against Mycobacterium tuberculosis (MTB). Two ether (3 and 4b) and one diamine (8b) derivatives have displayed high mycobactericidal potency, with similar MIC values of 1.25 μg/mL, against the virulent strain H37Rv, as well as against a clinical isolate resistant to the five first-line anti-TB drugs. The three compounds, tested on other eleven cultured MTB strains with different multi-drug-resistance (MDR) patterns, retained their MIC values for most strains, or even lowered it, as in the case of compound 4b, which, assayed on strain No. 332, also resistant to all first-line anti-TB drugs, attained the MIC value of 0.78 μg/mL.
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.
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 (2007/10/03)
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.
