3624-90-6Relevant articles and documents
Group 4 metal complexes containing the salalen ligands: Synthesis, structural characterization and studies on the ROP of cyclic esters
Chakraborty, Debashis,Rajashekhar, Bijja,Mandal, Mrinmay,Ramkumar, Venkatachalam
, p. 111 - 121 (2018)
The synthesis of homoleptic salalen ligand supported group 4 complexes and their applications in the ring-opening polymerization (ROP) of ε-caprolactone (?-CL) and lactide (LA) are described. All these complexes of type M(L)2 (LH = (E)-N-(2-(3,
Fe-based metal-organic frameworks for the synthesis of N-arylsulfonamides via the reactions of sodium arylsulfinates or arylsulfonyl chlorides with nitroarenes in water
Li, Xinxin,Chen, Fei,Lu, Guo-Ping
supporting information, p. 4226 - 4230 (2018/10/26)
A newly developed chemoselective reaction of sodium arylsulfinates or arylsulfonyl chlorides with nitroarenes has been disclosed. The chemistry, in which non-toxic water and recyclable iron-based metal-organic frameworks are employed as the solvent and catalyst, respectively, provides an efficient approach for the generation of N-arylsulfonamides, which are widely present in biologically active compounds and drugs, rendering this methodology attractive to both synthetic and medicinal chemistry.
A novel serine racemase inhibitor suppresses neuronal over-activation in vivo
Mori, Hisashi,Wada, Ryogo,Takahara, Satoyuki,Horino, Yoshikazu,Izumi, Hironori,Ishimoto, Tetsuya,Yoshida, Tomoyuki,Mizuguchi, Mineyuki,Obita, Takayuki,Gouda, Hiroaki,Hirono, Shuichi,Toyooka, Naoki
, p. 3736 - 3745 (2017/06/13)
Serine racemase (SRR) is an enzyme that produces D-serine from L-serine. D-Serine acts as an endogenous coagonist of NMDA-type glutamate receptors (NMDARs), which regulate many physiological functions. Over-activation of NMDARs induces excitotoxicity, which is observed in many neurodegenerative disorders and epilepsy states. In our previous works on the generation of SRR gene knockout (Srr-KO) mice and its protective effects against NMDA- and Aβ peptide-induced neurodegeneration, we hypothesized that the regulation of NMDARs’ over-activation by inhibition of SRR activity is one such therapeutic strategy to combat these disease states. In the previous study, we performed in silico screening to identify four compounds with inhibitory activities against recombinant SRR. Here, we synthesized 21 derivatives of candidate 1, one of four hit compounds, and performed screening by in vitro evaluations. The derivative 13J showed a significantly lower IC50 value in vitro, and suppressed neuronal over-activation in vivo.