| 摘要 |
A class of 3-phenylimidazo(1,2-a)pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein Y represents a chemical bond, an oxygen atom, or a -NH- linkage; Z represents an optionally substituted aryl or heteroaryl group; R<1 >represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, -OR<a>, -SR<a>, -SOR<a>, -SO2R<a>, -SO<2>NR<a>R<b>, -NR<a>R<b>, -NR<a>COR<b>, -NR<a>CO2R<b>, -COR<a>, CO2R<a>, -CONR<a>R<b >or -CR<a>=NOR<b>; and R<a >and R<b >independently represent hydrogen, hydrocarbon or a heterocyclic group.), substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, are selective ligands for GABAA receptors, in particular having good affinity for the a2 and/or a3 and/or a5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
|
