| 摘要 |
<p>Oxadiazoles represented by structural formula I: <CHEM> or a salt or prodrug thereof; wherein one of X, Y or Z is an oxygen atom and the other two are nitrogen atoms, and the dotted circle represents aromaticity (two double bonds); R<2> represents a substituent of low lipophilicity; the broken line represents an optional chemical bond; and the substituents R<3> and R<4> may be present at any position, including the point of attachment to the oxadiazole ring, and R<3> represents halo, C1-4 alkoxy, carboxy, -NR<7>R<8>, C2-4 alkyl, C1-4 alkyl substituted with hydroxy or C1-4 alkoxy, or methyl or hydroxy in the 3-, 4- or 5-position; and R<4> represents hydrogen, halo, C1-4 alkoxy, hydroxy, carboxy, -NR<7>R<8>, C1-4 alkyl, or C1-4 alkyl substituted with hydroxy or C1-4 alkoxy; or R<3> and R<4> together represent carbonyl; and R<7> and R<8> independently represent hydrogen or C1-2 alkyl are potent muscarinic agonists with good CNS penetrability, and are therefore useful in the treatment of neurological and mental illnesses; the compounds are also of benefit in the treatment of severe painful conditions. Processes for preparing these compounds are described, as also are pharmaceutical compositions containing them.</p> |
