- 1,3-Disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors
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In a search for novel DPP-IV inhibitors, 2-aminobenzo[a]quinolizines were identified as submicromolar HTS hits. Due to the difficult synthetic access to this compound class, 1,3-disubstituted 4-aminopiperidines were used as model compounds for optimizatio
- Luebbers, Thomas,Boehringer, Markus,Gobbi, Luca,Hennig, Michael,Hunziker, Daniel,Kuhn, Bernd,Loeffler, Bernd,Mattei, Patrizio,Narquizian, Robert,Peters, Jens-Uwe,Ruff, Yves,Wessel, Hans Peter,Wyss, Pierre
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p. 2966 - 2970
(2008/02/11)
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- Synthesis and Antihypertensive Activity of a Series of Spiroquinolizine-2,5'-oxazolidin-2'-one>s
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The 2R*,11bS* and 2S*,11bS* diastereoisomers of the spiroquinolizine-2,5'-oxazolidin-2'-one> system were prepared by stereoselective methods.Evaluation of these compounds for antihypertensive activity by oral administration to the spontaneously hypertensive rat showed the 2S*,11bS* series was the more potent.Within that series it was found that small alkyl substituents at positions 3 and 4' enhanced antihypertensive activity and that methoxyl substitution at positions 9 and 10 was optical. (2S,3S,11bS)-Spiroquinolizine-2,5'-oxazolidin-2'-one> was one of the most efficacious compounds of this series, while its antipode, (+)-9e, was inactive.Selected compounds in this series were shown to be α-adrenoceptor antagonists.
- Caroon, Joan M.,Clark, Robin D.,Kluge, Arthur F.,Lee, Chi-Ho,Strosberg, Arthur M.
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p. 1426 - 1433
(2007/10/02)
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