90340-70-8Relevant academic research and scientific papers
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: Discovery of potent water-soluble calpain inhibitors with oral bioavailability
Lubisch, Wilfried,Beckenbach, Edith,Bopp, Sabina,Hofmann, Hans-Peter,Kartal, Arzu,K?stel, Claudia,Lindner, Tanja,Metz-Garrecht, Marion,Reeb, Jutta,Regner, Ferdinand,Vierling, Michael,M?ller, Achim
, p. 2404 - 2412 (2007/10/03)
Novel benzoylalanine-derived ketoamides were prepared and evaluated for calpain I inhibition. Derivatives carrying vinylbenzyl amino residues in the P2 - P3 region inhibited calpain in nanomolar concentrations and thus represent a novel class of nonpeptidic calpain inhibitors. Selected examples exhibited an improved pharmacokinetic profile including improved watersolubility and metabolic stability. In particular, these calpain inhibitors showed oral bioavailability in rats as demonstrated by N-(1-benzyl-2-carbamoyl-2-oxoethyl)-2- [E-2-(4-diethylaminomethylphenyl)ethen-1-yl]benzamide (5d). The closely related derivative N-(1-carbamoyl-1-oxohex-1-yl)-2-[E-2- (4-dimethylaminomethylphenyl)-ethen-1-yl]benzamide (5b) was evaluated for neuroprotective efficacy after experimental traumatic brain injury in a fluid percussion model in rats. When administered after injury, 5b reduced the number of damaged neurons by 41%, and this result would be in line with the suggested neuroprotective efficacy of calpain inhibition.
Benzamidoaldehydes and their use as cysteine protease inhibitors
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, (2008/06/13)
Compounds of the formula where R1, R2, R3, X and n are as defined in the description, are inhibitors of cysteine protease.
The Photochemistry of Alkyl 2-(Naphthalenyl)ethenylbenzoates:Photodehydrocyclization and Photodimerization Products and Their Structural Elucidation by 1H and 13C N.M.R.
Jones, Alan J.,Teitei, Tsutomu
, p. 561 - 576 (2007/10/02)
Irradiation of alkyl 2-benzoates in benzene gave the photodehydrocyclization product, the chrysenecarboxylates (3) as well as two of the photodimerization products, the cyclobutanes (6) and (7).Similarly, irradiation of alkyl 2
