Madsen, Ulf; Brehm, Lotte; Schaumburg, Kjeld; Joergensen, Flemming S.; Krogsgaard-Larsen, Povl published an article on January 31 ,1990. The article was titled 《Relationship between structure, conformational flexibility, and biological activity of agonists and antagonists at the N-methyl-D-aspartic acid subtype of excitatory amino acid receptors》, and you may find the article in Journal of Medicinal Chemistry.Application In Synthesis of Cis-piperidine-2,6-dicarboxylic acid The information in the text is summarized as follows:
The relationship between conformational flexibility and agonist or antagonist actions at the N-methyl-D-aspartic acid (NMDA) subtype of central L-glutamic acid (GLU) receptors of a series of racemic piperidinedicarboxylic acids (PDAs) was studied. The conformational analyses were based on 1H NMR spectroscopy and supported by computer simulations and mol. mechanics calculations While the trans-forms of 2,3-PDA and 2,4-PDA and cis-2,5-PDA show NMDA receptor agonist activities, cis-2,3-PDA and cis-2,4-PDA are NMDA antagonists. The compounds trans-2,5-PDA and cis-2,6-PDA did not interact with NMDA receptors. Each of the 3 cyclic acidic amino acids showing NMDA agonist activities existed as an equilibrium mixture of 2 conformers in aqueous solution In contrast, the NMDA antagonists cis-2,3-PDA and cis-2,4-PDA as well as the inactive compounds trans-2,5-PDA and cis-2,6-PDA exist predominantly in a single conformation. These results seem to indicate that a certain degree of conformational flexibility of analogs of GLU is prerequisite for activation of, but not for binding to, the NMDA receptor. The results came from multiple reactions, including the reaction of Cis-piperidine-2,6-dicarboxylic acid(cas: 59234-40-1Application In Synthesis of Cis-piperidine-2,6-dicarboxylic acid)
Cis-piperidine-2,6-dicarboxylic acid(cas: 59234-40-1) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Application In Synthesis of Cis-piperidine-2,6-dicarboxylic acid
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem