| 摘要 |
Compounds of formula (I), wherein Ar<1> and Ar<2> are independently phenyl unsubstituted or substituted by halogen, hydroxy, thiol, lower alkoxy, lower thioalkyl, lower alkanoyloxy, lower alkyl, nitro, amino, lower S(O)n-alkyl wherein n is 0, 1, or 2, sulfonamide or trifluoromethyl; or a heteroaryl selected from 2- or 3-thienyl or 2- or 3-furanyl wherein the thienyl or furanyl is unsubstituted or substituted by lower alkyl, or halogen; with the overall proviso that at least one of Ar<1> or Ar<2> is the heteroaryl and that both of Ar<1> and Ar<2> cannot have more than one substitution; R2', R3', and R5' are each independently hydrogen, alkanoyl having two to twelve carbon atoms in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; additionally, R2' and R3' may be linked together to form a five-membered alkylidene ring having a total of up to twenty carbons such as, for example, isopropylidene, or a cyclic phosphate ester and R5' may be a phosphate, hydrogen or dihydrogen phosphate, or an alkali metal or ammonium or dialkali or diammonium salt thereof, such as, for example, PO3Na2. The novel 2- or 3-thienyl and 2- or 3-furanyl derivatives of adenosines of the present invention provide very potent A1 and A2 selective receptor binding activity. Particularly, the present invention provides highly active antipsychotic and advantageous cardiovascular effects. |
