Cysteine Derivatives as Inhibitors for Carboxypeptidase A: Synthesis and Structure−Activity Relationships
摘要:
A series of cysteine (Cys) derivatives having an alkyl or arylalkyl moiety on the a-amino group of the amino acid have been synthesized as a novel type of inhibitor for carboxypeptidase A. These compounds are readily prepared starting with Cys in an optically active form. The structure-activity relationship study revealed that the inhibitors prepared from D-Cys are much more potent than the corresponding inhibitors obtained from L-CYS, and the most potent inhibitor in the series, (S)-1j with a K-i value of 55 +/- 4 nM, is obtained by introducing a phenethyl moiety on the amino group Of D-CyS. In comparison, the most active inhibitor in the series of 2-substituted 3-mercaptopropanoic acid is found to be 20, in which the phenyl ring is linked to the mercaptocarboxylic acid at the a-position with a methylene unit. A proposal that accounts for the different structural requirement for the maximum activity between the two series of inhibitors is provided.
The present technology relates to compounds, kits, compositions, and methods useful for the treatment of numerous pathologies including dementia, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, and other neurodegenerative diseases, spinal cord injury, traumatic brain injury, diabetes and metabolic syndrome, defective wound healing, and/or sensorineural hearing and vision loss.
[EN] COMPOSITIONS USEFUL IN THERAPY OF AUTOPHAGY-RELATED PATHOLOGIES, AND METHODS OF MAKING AND USING THE SAME<br/>[FR] COMPOSITIONS UTILES EN THÉRAPIE DE PATHOLOGIES LIÉES À L'AUTOPHAGIE, ET LEURS PROCÉDÉS DE FABRICATION ET D'UTILISATION
申请人:UNIV TOLEDO
公开号:WO2017147440A1
公开(公告)日:2017-08-31
Lanthionine ketimine derivatives, and methods of making and using the same, are described. Included are lanthionine ketimine phosphonate (LK-P), lanthionine ketimine ester phosphonate (LKE-P) derivatives, as well as lanthionine ketimine derivatives having a tert-enamide moiety at the 2-position (NVP-LKE).
PROCESS FOR THE PREPARATION OF 3,4-DISUBSTITUTED-THIAZOLIDIN-2-ONES
申请人:DeCamp Jonathan B.
公开号:US20070225504A1
公开(公告)日:2007-09-27
The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.
The present invention relates to a method of preparation of an optically active cyclohexenone derivative of Formula (I) O R 1 R 2 * R 1 and wherein R1 and R2 are organic residues.
[EN] NOVEL COMPOUNDS WITH DUAL ACTIVITY<br/>[FR] NOUVEAUX COMPOSÉS À DOUBLE ACTIVITÉ
申请人:YISSUM RES DEV CO
公开号:WO2017042805A1
公开(公告)日:2017-03-16
The invention generally relate to novel compounds and uses thereof in preventing antifouling by unicellular organisms and in attracting cells from multicellular organisms.