Preparation of tetrahydroimidazo[2,1-a]isoquinolines and their use as inhibitors of gastric acid secretion |
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| Authors: | Palmer Andreas Marc Grobbel Burkhard Brehm Christof Zimmermann Peter Jan Buhr Wilm Feth Martin Philipp Holst Hans Christof Simon Wolfgang Alexander |
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| Affiliation: | aNYCOMED GmbH, Byk-Gulden-Str. 2, D-78467 Konstanz, Germany |
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| Abstract: | A series of novel tetrahydroimidazo[2,1-a]isoquinolines was prepared based on a hetero Diels–Alder reaction between an enamine and 1,2,4-triazine as key step. A structure–activity relationship was established focussing on the influence of the substitution pattern in position 3 and 6 of the heterocycle on antisecretory activity, lipophilicity, and pKa value. Potent inhibitors of the gastric acid pump were identified. |
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| Keywords: | Hetero Diels–Alder reaction Tetrahydroimidazo[2,1-a]isoquinolines Antisecretory activity Gastric acid pump H+/K+-ATPase |
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