| 摘要 |
<p>Trifluoromethyl oligopeptides of formula (I) are new. CF3CO-X-Y-NH-(CH2 )n (1) (-X-Y-is-Ala-Ala; n is 0; R is H, m-NO2, p-Cl, p-CF3, p-OMe, p-iPr, p-CN or p-CO2H; or -X-Y- is -Lys-Ala-; n is 0 (but can also be 1 when R is H); R is p-CF3, p-Me, p-iPr, p-NMe2, p-COMe, p-iBu, p-cyclohexyl, p-F, p-NEt2 or H; or -X-Y- is -Ala-DL-NHCH(CF3)CO-; n is 0, R is H; or -X-Y- is -Lys-Lys or -Ala-Lys-; n is 0; R is p-CF3; or -X-Y- is -Lys-Pro-, -Lys-Phe-, -Lys-Val- or -Lys-Leu-; n is 0; R is iPr). (I) are reversible inhibitors of leukocytic and pancreatic elastases. In 0.2M Tris buffer, pH 8, 25 degrees, inhibitory concns. are 2.5 x 10-8 - 5.5 x 10-7M for pancreatic and 3 x 10-7 - 4.4 x 10-5M for leukocytic elastases. The range of I50 values for the latter is 5.7 x 10-6 - 4.7 x 10-4M. (I) can be used as drugs, e.g. for treating emphysema.</p> |
