| 摘要 |
<p>New N-acyl homoserine lactone compounds of the formula (I) in whichR is an acyl group of the formula (II) wherein one of R?1 and R2¿ is H and the other is selected from OR4, SR4 and NHR4, wherein R4 is H or 1-6C alkyl, or R?1 and R2¿ together with the carbon atom to which they are joined form a keto group, and R3 is a straight or branched chain, saturated or unsaturated aliphatic hydrocarbyl group containing from 8 to 11 carbon atoms and is optionally substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl, carbamoyl optionally mono- or disubstituted at the N atom by 1-6C alkyl and NR5R6 wherein each of R?5 and R6¿ is selected from H and 1-6C alkyl or R?5 and R6¿ together with the N atom form a morpholino or piperazino group, or any enantiomer thereof, with the proviso that R is not a 3-oxododecanoyl group, having immunosuppressant properties are disclosed. The compounds are shown to have an inhibitory effect on lymphocyte proliferation and down-regulate TNF-α secretion by monocytes/macrophages in the animal body, including the human body. Pharmaceutical compositions comprising N-acyl homoserine lactones are also described.</p> |
