140211-12-7Relevant academic research and scientific papers
Synthesis of Fused Bicyclic Piperidines: Potential Bioactive Templates for Medicinal Chemistry
Zhou, Jinglan,Campbell-Conroy, Erica L.,Silina, Alina,Uy, Johnny,Pierre, Fabrice,Hurley, Dennis J.,Hilgraf, Nicole,Frieman, Bryan A.,DeNinno, Michael P.
, p. 70 - 79 (2015)
An array of six pyridyl-substituted fused bicyclic piperidines was prepared as novel cores for medicinal chemistry. For maximum diversity, the size of the fused ring varied from three to six atoms and contained up to two oxygen atoms. The pyridine ring was incorporated to improve physicochemical properties and to challenge the robustness of the chemistry. The presence of the pyridine did interfere with our initial approaches to these molecules, and in several instances, a blocking strategy had to be employed. These new scaffolds possess high sp3 character and may prove useful in multiple medicinal chemistry applications.
FUSED PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
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Paragraph 00211; 00212, (2015/02/02)
The invention relates to fused piperidine amides useful as inhibitors of ion channels for the treatment of pain. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Synthesis and antibacterial activity of new 7-(aminoazabicycloalkanyl)quinolonecarboxylic acids
Ogata, M,Matsumoto, H,Shimizu, S,Kida, S,Nakai, H,et al.
, p. 889 - 906 (2007/10/02)
A series of novel 7--6-fluoro-1-substituted quinolinecarboxylic acids (18-53) have been prepared and their antibacterial activities evaluated.These compounds are characterized structurally by a new amino-substituted azabicyclooctane, -nonane and -decane ring systems at the 7-position of quinolonecarboxylic acids.To compare the biological activities of enantiomers, (+)-7-octan-3-yl>-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolonecarboxylicacid hydrochloride (43, 44) were synthesized and evaluated for antibacterial activity.Compound 43 was more potent than 44 against both Gram-positive and Gram-negative organisms.The structure-activity relationships of these quinolonecarboxylic acids are also discussed. antibacterial activity / amino-substituted azabicycloalkane ring / substituted quinolonecarboxylic acids / structure-activity relationships
