155778-26-0Relevant academic research and scientific papers
3-Amidoquinuclidine derivatives: Synthesis of compounds and inhibition of butyrylcholinesterase
Odzak, Renata,Tomic, Srdanka
, p. 90 - 98 (2006)
The synthesis of racemic and enantiomerically pure 3- butanamidoquinuclidines ((±)-Bu, (R)-Bu and (S)-Bu), (1-3) and 3-benzamidoquinuclidines ((±)-Bz, (R)-Bz, and (S)-Bz), (4-6) is described. The N-quaternary derivatives, N-benzyl-3-butanamidoquinuclidinium bromides ((±)-BnlBu, (R)-BnlBu and (S)-BnlBu), (7-9) and N-benzyl-3-benzamidoquinuclidinium bromides ((±)-BnlBz, (R)-BnlBz and (S)-BnlBz), (10-12) were subsequently synthesized. The interaction of the four enantiomerically pure quaternary derivatives with horse serum butyrylcholinesterase (BChE) was tested. All tested compounds inhibited the enzyme. The best inhibitior of the enzyme was (S)-BnlBz with a Ki = 3.7 μM. The inhibitor potency decreases in order (S)-BnlBz > (R)-BnlBz ? (R)-BnlBu > (S)-BnlBu.
HETEROCYCLIC DERIVATIVES AS M3 MUSCARINIC RECEPTORS
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Page/Page column 80, (2008/12/08)
This invention relates to M3 antagonists of formula (I) wherein R2, R4, R5, R6, W, V, A, D, X, t, u and v are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of diseases where enhanced M3 receptor activation is implicated.
