Abstract
A new series of 2,8-disubstituted-2,8-diazaspiro[4,5]decan-1-ones 2 has been synthesized and tested for affinity towards muscarinic receptors by binding studies in comparison with the model RS-86. The membrane phosphatidylinositol turnover in the presence or absence of carbachol has also been investigated. In both experiments all the new derivatives 2 were found to be less active than the model; only 5g, which retains the imidic moiety, could approach it in potency. A possible explanation for the lack of activity of this class of compounds is given in terms of the computed interaction energies of the minimized ligand-m1 receptor complex.
Original language | English |
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Pages (from-to) | 955-961 |
Number of pages | 7 |
Journal | European Journal of Medicinal Chemistry |
Volume | 29 |
Issue number | 12 |
DOIs | |
Publication status | Published - 1994 |
Externally published | Yes |
Keywords
- 2,8-disubstituted-2,8-diazaspiro[4,5]decan-1-one
- QSAR
- RS-86
- muscarinic agonist