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J Med Chem. 1992 Apr 3;35(7):1280-90.

Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.

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SmithKline Beecham Pharmaceuticals, Medicinal Research Centre, Harlow, Essex, U.K.


The synthesis of 15 methyl or unsubstituted 1,2,3-triazoles, 1,2,4-triazoles, and tetrazoles additionally substituted with a 1-azabicyclo[2.2.2]octan-3-yl group is described. The potency and efficacy of these compounds as muscarinic ligands were determined in radioligand binding assays using [3H]oxotremorine and [3H]quinuclidinyl benzilate. Potency and efficacy were found in compounds in which the azole moiety was attached to the azabicyclic ring either through a carbon atom or a nitrogen atom. Electrostatic potential maps of both the C-linked and the novel N-linked series of compounds were calculated. A relationship between position and depth of the electrostatic minima relative to the azabicyclic ring and the potency and efficacy of the compounds was determined.

[Indexed for MEDLINE]

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