858213-13-5Relevant articles and documents
Microwave assisted synthesis of indole derivatives, an their complexation behaviour and biological studies
Khan, M. Asif,Ahmad, Shamim
, p. 1061 - 1065,5 (2020/08/24)
Indole 2-Carboxyllic acid on condensation with benzene sulfonyl hydrazide gives the condensation product - Schiff base. This has been characterized by analytical data I.R. N.M.R. spectra. The complexes of Schiff base have been prepared with metals Mn (III), V (III), Co (III), Ti (III) and Fe (III). The complexes has been characterized by elemental analyses, I,R., 1H N.M.R., electronic spectra, molar conductance and Magnetic susceptibilities. These studies suggested Octahedral geometry around the respective metal ions. The ligand and its metal complexes have been screened for their biological activity.
The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases
Hu, Lain-Yen,Boxer, Peter A.,Kesten, Suzanne R.,Lei, Huangshu J.,Wustrow, David J.,Moreland, David W.,Zhang, Liming,Ahn, Kay,Ryder, Todd R.,Liu, Xiaohong,Rubin, John R.,Fahnoe, Kelly,Carroll, Richard T.,Dutta, Satavisha,Fahnoe, Douglass C.,Probert, Albert W.,Roof, Robin L.,Rafferty, Michael F.,Kostlan, Catherine R.,Scholten, Jeffrey D.,Hood, Molly,Ren, Xiao-Dan,Schielke, Gerald P.,Su, Ti-Zhi,Taylor, Charles P.,Mistry, Anil,McConnell, Patrick,Hasemann, Charles,Ohren, Jeffrey
, p. 2337 - 2340 (2007/10/03)
The inhibition of the cytosolic isoenzyme BCAT that is expressed specifically in neuronal tissue is likely to be useful for the treatment of neurodegenerative and other neurological disorders where glutamatergic mechanisms are implicated. Compound 2 exhibited an IC50 of 0.8 μM in the hBCATc assays; it is an active and selective inhibitor. Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective efficacy in vivo. SAR, pharmacology, and the crystal structure of hBCATc with inhibitor 2 are described.
