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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.

The acetyl group of the muscarinic agonist aceclidine 4 was replaced by various 1,2,5-thiadiazoles to provide a new series of potent m1 muscarinic agonists 17 and 18. Optimal m1 muscarinic agonist potency was achieved when the 1,2,5-thiadiazole substituent was either a butyloxy, 17d, or butylthio, 18d, group. Although 1,2,5-oxadiazole 37 and pyrazine 39 are iso-pi-electronic with 1,2,5-thiadiazole 17d, both analogues were substantially less active than 17d. Compounds with high muscarinic affinity and/or m1 muscarinic agonist efficacy were also obtained when the 3-oxyquinuclidine moiety of 17d or 18c was replaced by ethanolamines, hydroxypyrrolidines, hydroxyazetidine, hydroxyisotropanes, or hydroxyazanorbornanes. The structure-activity data support the participation of the oxygen or sulfur atom in the substituent on the 1,2,5-thiadiazole in the activation of the m1 receptor. Several of these new 1,2,5-thiadiazoles have m1 agonist efficacy, potency, and selectivity comparable to those of xanomeline 2 in the muscarinic tests investigated.[1]

References

  1. 1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists. Ward, J.S., Merritt, L., Calligaro, D.O., Bymaster, F.P., Shannon, H.E., Mitch, C.H., Whitesitt, C., Brunsting, D., Sheardown, M.J., Olesen, P.H., Swedberg, M.D., Jeppesen, L., Sauerberg, P. J. Med. Chem. (1998) [Pubmed]
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