2416-20-8Relevant articles and documents
NOVEL GLYCINE TRANSPORT INHIBITORS FOR THE TREATMENT OF PAIN
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Page/Page column 54; 55, (2018/08/12)
The present invention relates to novel glycine transport inhibitor compounds and their use for treating pain.
Synthesis and Characterization of Novel Acyl-Glycine Inhibitors of GlyT2
Mostyn, Shannon N.,Carland, Jane E.,Shimmon, Susan,Ryan, Renae M.,Rawling, Tristan,Vandenberg, Robert J.
, p. 1949 - 1959 (2017/09/26)
It has been demonstrated previously that the endogenous compound N-arachidonyl-glycine inhibits the glycine transporter GlyT2, stimulates glycinergic neurotransmission, and provides analgesia in animal models of neuropathic and inflammatory pain. However, it is a relatively weak inhibitor with an IC50 of 9 μM and is subject to oxidation via cyclooxygenase, limiting its therapeutic value. In this paper we describe the synthesis and testing of a novel series of monounsaturated C18 and C16 acyl-glycine molecules as inhibitors of the glycine transporter GlyT2. We demonstrate that they are up to 28 fold more potent that N-arachidonyl-glycine with no activity at the closely related GlyT1 transporter at concentrations up to 30 μM. This novel class of compounds show considerable promise as a first generation of GlyT2 transport inhibitors.
Kolbe Synthesis of Unsaturated Pheromones by Coelectrolysis with 5-Alkynoic Acids
Seidel, Wolfgang,Schaefer, Hans J.
, p. 3898 - 3903 (2007/10/02)
The alkynoic acids 5a - g are synthesized by coelectrolysis of 5-alkynoic acids 2a - c with dicarboxylic monoesters 3a - d.By reduction, Lindlar-hydrogenation, and acetylation these are converted into pheromones such as (Z)-11-hexadecenyl acetate (7b), the pheromone of Mamestra brassicae. 2a - c can be prepared by alkynylation of 1-bromo-3-chloropropane to 1a - c, substitution by cyanide and hydrolysis.
