6288-14-8Relevant articles and documents
Design, synthesis, and evaluation of novel inhibitors for wild-type human serine racemase
Takahara, Satoyuki,Nakagawa, Kiyomi,Uchiyama, Tsugumi,Yoshida, Tomoyuki,Matsumoto, Kazunori,Kawasumi, Yasuo,Mizuguchi, Mineyuki,Obita, Takayuki,Watanabe, Yurie,Hayakawa, Daichi,Gouda, Hiroaki,Mori, Hisashi,Toyooka, Naoki
supporting information, p. 441 - 445 (2017/12/28)
Most of the endogenous free D-serine (about 90%) in the brain is produced by serine racemase (SR). D-Serine in the brain is involved in neurodegenerative disorders and epileptic states as an endogenous co-agonist of the NMDA-type glutamate receptor. Thus, SR inhibitors are expected to be novel therapeutic candidates for the treatment of these disorders. In this study, we solved the crystal structure of wild-type SR, and tried to identify a new inhibitor of SR by in silico screening using the structural information. As a result, we identified two hit compounds by their in vitro evaluations using wild-type SR. Based on the structure of the more potent hit compound 1, we synthesized 15 derivatives and evaluated their inhibitory activities against wild-type SR. Among them, the compound 9C showed relatively high inhibitory potency for wild-type SR. Compound 9C was a more potent inhibitor than compound 24, which was synthesized by our group based upon the structural information of the mutant-type SR.
Preparation and use of (S)-O-acetyllactyl chloride (Mosandl's reagent) as a chiral derivatizing agent
Buisson, Didier,Azerad, Robert
, p. 2997 - 3002 (2007/10/03)
(S)-O-Acetyllactyl chloride is used as a versatile chiral derivatizing agent for the chromatographic determination of the enantiomeric excesses of alcohols or amines. However, some precautions must be taken to avoid its racemization during preparation and use. In addition, the racemic counterpart of this reagent can be used to determine the best analytical separation conditions.