S. Scapecchi et al., SAR STUDIES ON THE POTENT AND SELECTIVE MUSCARINIC ANTAGONIST 2-ETHYLTHIO-2,2-DIPHENYLACETIC ACID N,N-DIETHYLAMINOETHYL ESTER, Archiv der pharmazie, 330(5), 1997, pp. 122-128
Molecular modification of the potent and selective muscarinic antagoni
st 2-thylthio-2,2-diphenylacetic acid N,N-diethylaminoethyl ester was
performed in order to identify M-2 selective antagonists able to cross
the blood brain barrier and potentially useful in the treatment of Al
zheimer's disease. Modifications included substitution or hydrogenatio
n of one of the phenyl rings as well as their incorporation in a tricy
clic system. In general the changes introduced were detrimental for bo
th affinity and selectivity. Only a modest M-2 selectivity is present
in some compounds that, on the other hand, carry a quaternary ammonium
group which precludes their penetration into the brain.