Synthesis of conformationally constrained analogues of BRL32872 : Determination of stereochemistry and related pharmacological properties

Souchet, M., Forest, M.-C., Cheval, B., Rouanet, S., Faivre, J.-F., Bril, A., Gerhard, U. and Smith, R.J. (1997) Synthesis of conformationally constrained analogues of BRL32872 : Determination of stereochemistry and related pharmacological properties. Bioorganic and Medicinal Chemistry Letters (15). pp. 1989-1994. ISSN 0960-894X
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2-Azabicyclo[2.2.2]octane derivatives have been used as conformationally constrained structure of BRL-32872, in order to investigate the effect of molecular flexibility towards class III and class IV antiarrhythmic properties. Extensive NMR studies allowed the determination of the configuration at C5. Stereoisomerism induces variability of biological profile.

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