Quinlobelane: a water-soluble lobelane analogue and inhibitor of VMAT2.

ID: ALA1158628

Journal: Bioorg Med Chem Lett

Title: Quinlobelane: a water-soluble lobelane analogue and inhibitor of VMAT2.

Authors: Vartak AP, Gabriela Deaciuc A, Dwoskin LP, Crooks PA.

Abstract: Replacing the phenyl groups in the structure of the VMAT2 inhibitor, lobelane with either pyridyl, quinolyl or indolyl groups affords novel analogues with improved water solubility. The synthetic methodologies reported herein also underscore the paucity of hydrogenation methods that offer selectivity in the synthesis of the different classes of heteroaromatic lobelane analogues. The quinolyl group was the only replacement for the phenyl group in lobelane that retained VMAT2 inhibition.

CiteXplore: 20494575

DOI: 10.1016/j.bmcl.2010.04.117

Patent ID: ┄