Is a nitrogen atom an important pharmacophoric element in sigma ligand binding?
S Y Ablordeppey, J B Fischer, R A Glennon
文献索引：Bioorg. Med. Chem. 8(8) , 2105-11, (2000)
全文：HTML全文
摘要
A lingering question in sigma receptor ligand development is whether a nitrogen atom serves as an important pharmacophoric element in binding affinity. To address this question, we have synthesized several phenylalkylpiperidines and phenylalkylpiperazines and demonstrated that removal of the N atom from a typical phenylalkylpiperidine led to little or no binding to sigma receptors. In addition, where two N atoms occur in a compound, such as with phenylalkylpiperazines, the N atom on the longer alkyl chain appears to be more important. Thus, based on this study, the N atom is an important pharmacophoric element in the binding of phenylalkylpiperidines and phenylalkylpiperazines to sigma receptors.