696-75-3Relevant articles and documents
HETEROCYCLIC COMPOUNDS AS ARGINASE INHIBITORS
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Page/Page column 65, (2019/07/13)
The present invention relates to heterocyclic compounds as arginase inhibitors, in particular to a compound represented by Formula (I), or a pharmaceutically acceptable salt, stereoisomer or tautomer, or prodrug thereof and a pharmaceutical composition comprising said compound.
Cyclopropane derivatives as potential human serine racemase inhibitors: Unveiling novel insights into a difficult target
Beato, Claudia,Pecchini, Chiara,Cocconcelli, Chiara,Campanini, Barbara,Marchetti, Marialaura,Pieroni, Marco,Mozzarelli, Andrea,Costantino, Gabriele
, p. 645 - 652 (2016/05/09)
d-Serine is the co-agonist of NMDA receptors and binds to the so-called glycine site. d-Serine is synthesized by human serine racemase (SR). Over activation of NMDA receptors is involved in many neurodegenerative diseases and, therefore, the inhibition of SR might represent a novel strategy for the treatment of these pathologies. SR is a very difficult target, with only few compounds so far identified exhibiting weak inhibitory activity. This study was aimed at the identification of novel SR inhibitor by mimicking malonic acid, the best-known SR inhibitor, with a cyclopropane scaffold. We developed, synthesized, and tested a series of cyclopropane dicarboxylic acid derivatives, complementing the synthetic effort with molecular docking. We identified few compounds that bind SR in high micromolar range with a lack of significant correlation between experimental and predicted binding affinities. The thorough analysis of the results can be exploited for the development of more potent SR inhibitors.
An efficient and improved process for the scale-up preparation of cis-cyclopropanediamine dihydrochloride
Wang, Fan,Xu, Xiao-Ying,Wang, Fei-Ying,Peng, Lin,Zhang, Yong,Wang, Liang-Liang,Wang, Li-Xin
, p. 741 - 744 (2016/03/25)
An effective and improved process for the preparation of cis-cyclopro panediamine dihydrochloride was developed in a 100 g scale. The key step in the process is the preparation of ciscyclopropane-1, 2-dicarboxylic acid from a mixture of cis- and transisomers by the formation of cyclic acidic anhydride. The whole process and all of the procedures are economical, industrially reliable and easily scaled up.
