Synthesis and evaluation of novel azetidine analogs as potent inhibitors of vesicular [3 H] dopamine uptake

D Ding, JR Nickell, AG Deaciuc, NR Penthala…

Index: Ding, Derong; Nickell, Justin R.; Deaciuc, Agripina G.; Penthala, Narsimha Reddy; Dwoskin, Linda P.; Crooks, Peter A. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 21 p. 6771 - 6777

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Citation Number: 3

Abstract

Abstract Lobelane analogs that incorporate a central piperidine or pyrrolidine moiety have previously been reported by our group as potent inhibitors of VMAT2 function. Further central ring size reduction of the piperidine moiety in lobelane to a four-membered heterocyclic ring has been carried out in the current study to afford novel cis-and trans- azetidine analogs. These azetidine analogs (15a–15c and 22a–22c) potently inhibited [3 ...