137172-67-9Relevant academic research and scientific papers
Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid
Einsiedel, Juergen,Weber, Klaus,Thomas, Christoph,Lehmann, Thomas,Huebner, Harald,Gmeiner, Peter
, p. 3293 - 3296 (2007/10/03)
Employing the achiral 4-aminopiperidine derivative clebopride as a lead compound, chiral analogues were developed displaying dopamine receptor binding profiles that proved to be strongly dependent on the stereochemistry. Compared to the D1 receptor, the t
Fluoronaphthyridines and -quinolines as Antibacterial Agents. 5. Synthesis and Antimicrobial Activity of Chiral 1-tert-Butyl-6-fluoro-7-substituted-naphthyridones
Cesare, P. Di,Bouzard, D.,Essiz, M.,Jacquet, J. P.,Ledoussal, B.,et al.
, p. 4205 - 4213 (2007/10/02)
A series of novel 7-substituted-1-tert-butyl-6-fluoronaphthyridone-3-carboxylic acids has been prepared.These derivatives are characterized by chiral aminopyrrolidine substituents at the 7 position.In this paper we report the full details of the asymmetric synthesis of this series of compounds.Structure-activity relationship studies indicate that the absolute stereochemistry at the asymmetric centers of the pyrrolidine ring is critical for maintaining good activity.Compounds 60 and 61 (3-amino-4-methylpyrrolidine enantiomers) were selected for preclinical evaluation.
Isoindoline derivatives
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, (2008/06/13)
Optically active 8-methoxyquinolonecarboxylic acids represented by the formula (I) wherein R1 is lower alkyl have been found to possess potent antibacterial activity against both Gram-negative and Gram-positive bacteria. The compounds may be synthesized from novel optically active intermediates.
