68165-06-0Relevant articles and documents
Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors
Bekkali, Younes,Thomson, David S.,Betageri, Raj,Emmanuel, Michel J.,Hao, Ming-Hong,Hickey, Eugene,Liu, Weimin,Patel, Usha,Ward, Yancey D.,Young, Erick R.R.,Nelson, Richard,Kukulka, Alison,Brown, Maryanne L.,Crane, Kathy,White, Della,Freeman, Dorothy M.,Labadia, Mark E.,Wildeson, Jessi,Spero, Denice M.
, p. 2465 - 2469 (2008/03/11)
The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue.
Chiral arylpyrrolidinols: Preparation and biological profile
Collina, Simona,Rossi, Daniela,Loddo, Guya,Barbieri, Annalisa,Lanza, Enrica,Linati, Laura,Alcaro, Stefano,Gallelli, Andrea,Azzolina, Ornella
, p. 3117 - 3126 (2007/10/03)
The preparation and biological evaluation of a new class of arylpyrrolidinols is reported. The antinociceptive activity was evaluated in vivo with the hot plate test (HPT) and formalin test (FT), excluding any involvement on motor coordination with the rota-rod test (RRT). The nociceptive behavior in the late phase of FT (representative of chronic pain) suggests an involvement of the antiinflammatory process and it is clearly influenced by the stereochemical features, being the eutomer of phenylpyrrolidinols, the (2R,3S) enantiomer. Despite this, a specific mechanism of action is not yet clarified.
6,7-dihydropyrrol[3,4-c]pyrido[2,3-d]pyrimidine derivatives
-
, (2008/06/13)
The present invention concerns compounds of the formula: STR1 wherein R is a lower alkyl group, an aryl group or an alkylaryl group and X and Y are the same or different, and each is OH, NH2, or SH. The aryl group or the aryl moiety of the alkylaryl group may be unsubstituted, monosubstituted, disubstituted or trisubstituted. If substituted, each substituent may independently be an alkyl group, an alkyloxy group or a halogen. The present invention also provides methods for synthesizing the compounds described above.
ON THE GIF OXIDATION OF ALICYCLIC TERTIARY AMINES
Barton, D.H.R,Boivin, J.,Gaudin D.,Jankowski, K.
, p. 1381 - 1382 (2007/10/02)
Oxidation of various tertiary amines by the GifIV system based on iron catalyst associated with a reductant (zinc) and molecular oxigen, led to a mixture of the keto-derivatives and the corresponding lactams.Steric hindrance and electron withdrawing substituents exert a deactivating effect on the oxidation.
N-Heterocyclic-9-xanthenylamines
-
, (2008/06/13)
The compounds are N-piperidinyl and pyrrolidinyl-9-xanthenylamines which are inhibitors of gastric acid secretion.