Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl) benzylamine with elucidation of bioactive conformation: discovery of 1, 4-diazabicyclo [ …

R Kolhatkar, CD Cook, SK Ghorai…

Index: Kolhatkar, Rohit B.; Ghorai, Sujit K.; George, Clifford; Reith, Maarten E. A.; Dutta, Aloke K. Journal of Medicinal Chemistry, 2003 , vol. 46, # 11 p. 2205 - 2215

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Citation Number: 14

Abstract

Our structure-activity relationship (SAR) study on piperidine analogues for monoamine transporters led to the development of a series of 3, 6-disubstituted piperidine derivatives, structurally constrained versions of flexible piperidine analogues, with preferential affinity for the dopamine transporter (DAT). In our attempt to further rigidify this structure to study influence of rigidity on binding and in vivo activity, we have developed a series of 4, 8- ...