- ISOINDOLINE COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE
-
Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta- associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.
- -
-
-
- NOVEL PROCESS FOR THE PREPARATION OF (R)-N-BENZYL-2-ACETAMIDO-3-METHOXYPROPIONAMIDE
-
The invention is a novel process for the preparation of lacosamide by employing novel intermediates of formula III and IV:
- -
-
Paragraph 0043
(2014/11/11)
-
- Synthesis of a novel series of 2,3,4-trisubstituted oxazolidines designed by isosteric replacement or rigidification of the structure and cytotoxic evaluation
-
We have previously reported on a study of the structure-activity relationship in a series of 2,3,4-substituted oxazolidines recently discovered by our group varying the substituent at the ring or stereochemistry of the oxazolidine ring. We discovered the cytotoxic and pro-apoptotic potential of compounds 1 and 2 with good selectivity against cancer cell lines. In the present study we describe the synthesis and cytotoxic evaluation against cancer cell lines (HL60, JURKAT, MDA-MB-231 and LNCaP) of a series of oxazolidines designed by isosteric replacement or rigidification of the oxymethylene spacer of compounds 1 and 2. Alkenes 3 and 4 retained the activity against MDA-MB-231 cells and they were more active on HL60, JURKAT and LNCaP cells. Considering LNCaP cells, E-isomer 4 was at least 7 times and about 3 times more potent than lead 1 and Z-isomer 3, respectively. Compound 4 exerted significant activity against LNCaP with IC50 in the low micromolar range (11 μM) without affecting VERO cells and PBMC proliferation (IC50 > 100 μM) indicating its low toxicity to normal cells.
- Andrade, Saulo F.,Teixeira, Claudia S.,Ramos, Jonas P.,Lopes, Marcela S.,Pdua, Rodrigo M.,Oliveira, Mnica C.,Souza-Fagundes, Elaine M.,Alves, Ricardo J.
-
p. 1693 - 1699
(2014/12/11)
-
- NMR characterization and conformational analysis of a potent papain-family cathepsin L-like cysteine protease inhibitor with different behaviour in polar and apolar media
-
We recently reported the synthesis, of a potent papain-family cathepsin L-like cysteine protease inhibitor, as new lead compound for the development of new drugs that can be used as antiprotozoal agents. The investigation of its conformational profile is
- Rotondo, Archimede,Ettari, Roberta,Zappalà, Maria,De Micheli, Carlo,Rotondo, Enrico
-
p. 337 - 343
(2015/01/16)
-
- Effects on polo-like kinase 1 polo-box domain binding affinities of peptides incurred by structural variation at the phosphoamino acid position
-
Protein-protein interactions (PPIs) mediated by the polo-box domain (PBD) of polo-like kinase 1 (Plk1) serve important roles in cell proliferation. Critical elements in the high affinity recognition of peptides and proteins by PBD are derived from pThr/pS
- Qian, Wenjian,Park, Jung-Eun,Liu, Fa,Lee, Kyung S.,Burke Jr., Terrence R.
-
p. 3996 - 4003
(2013/07/27)
-
- Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors
-
This paper describes the synthesis of a new class of peptidomimetic cysteine protease inhibitors based on a 1,4-benzodiazepine scaffold and on an electrophilic vinyl sulfone moiety. The former was introduced internally to a peptide sequence that mimics th
- Ettari, Roberta,Nizi, Emanuela,Di Francesco, Maria Emilia,Dude, Marie-Adrienne,Pradel, Gabriele,Vi?ík, Radim,Schirmeister, Tanja,Micale, Nicola,Grasso, Silvana,Zappalà, Maria
-
p. 988 - 996
(2008/09/19)
-
- Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents
-
The synthesis of a new class of peptidomimetics 1a-j, based on a 1,4-benzodiazepine scaffold and on a C-terminal aspartyl aldehyde building block, is described. Compounds 1a-j provided significant inhibitory activity against falcipains 2A and 2B (FP-2A an
- Micale, Nicola,Kozikowski, Alan P.,Ettari, Roberta,Grasso, Silvana,Zappalà, Maria,Jeong, Jong-Jin,Kumar, Ajay,Hanspal, Manjit,Chishti, Athar H.
-
p. 3064 - 3067
(2007/10/03)
-
- Synthesis of C-glycosyl amino acids: Scope and limitations of the tandem Tebbe/Claisen approach
-
Amino acids may be used as coupling partners for esterification with 3-hydroxy glycals as substrates for the tandem Tebbe/Claisen approach to the synthesis of C-glycosyl amino acids. Whilst esters of substituted α-amino acids do not successfully undergo T
- Chambers, David J.,Evans, Graham R.,Fairbanks, Antony J.
-
-
- Derivatives of glycinergic r(+)-2-amino-3-hydroxypropanoic acid
-
The use of R(+)-2-amino-3-hydroxypropanoic acid derivatives, nitrogen substituted by a (C1-C6)alkyl, (C3-C6)alkenyl, 3-oxo(C5-C6)alkyl, 3-oxo(C4-C6)alken-2-yl, phenyl(
- -
-
Page/Page column 5
(2008/06/13)
-