| 摘要 |
<p>Trifluorethanol derivs of formula (Z)(Z')N-Ar-C(Z"R)H-CF3. (I) and their acid-addn salts and optical isomers are new. In (I) Z is H, 1-6C alkyl, lower cycloalkyl, N-alkylpiperidino (sic), N-aralkyl-piperidino (sic), lower alkanoyl, or acyl derived from an acid of formula (II) or (III); E is lower alkyl, lower alkoxy, CN, CF3, CF3O, CF3S, alkylsulphonyl or halogen; n=0-3; A is CH, S, O or NH; and B is S, O, NH or CH=N; Z' is H or lower alkyl; Z" is 0 or S; Ar is a 5-7C monocyclic homocyclic aromatic gp. and R is H, lower alkyl or lower acyl. Cpds (I) are antiinflammatory agents (ED50 is approx. 150 mg/kg) analgesics (ED50=50-100 mg/kg; aspirin=150 mg/kg) and antipyretic agents (more active than paracetamol), with very low acute toxicity (LD50 is approx. 2000 mg/kg).</p> |
