| 摘要 |
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 R<2 >is H and the other is selected from OR<4>, SR<4 >and NHR<4>, wherein R<4 >is H or 1-6C alkyl, or R<1 >and R<2 >together with the carbon atom to which they are joined form a keto group, and R<3 >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 NR<5>R<6 >wherein each of R<5 >and R<6 >is selected from H and 1-6C alkyl or R<5 >and R<6 >together with the N atom form a morpholino or piperazino group, or and enantiomer thereof, with the proviso that R is not a 3-oxododecanoyl group, having immuosuppressant properties are disclosed. The compounds are shown to have an inhibitory effect on lymphocyte proliferation and down-regulate TNF-alpha secretion by monocytes/macrophages in the animal body, including the human body. Pharmaceutical composition comprising N-acyl homoserine lactones are also described. |
