Twenty new compounds derived from deoxycholic acid have been synthesi-Antlmlkrobiell wlrksame besisehe Cholanderivate zed They contain two basic functions: at C-24 (bemylamino, morpholino, diethanolamino, N,N-diethylethylenediamino, N-methylpipemzino) and at B-C-3 (amino, methylamino, ethylamino, benzylamino). The compounds showed interesting antimicrobial activity, as expressed in terms of the low M.I.C. values (0.9-31-pglml) against five Gram(+) and four Gram(-) snains, two fungi and one yeast. The compounds inhibit the production of a fluorescent pigment in Pseudomonar aeruginosa: this result suggests that the ability to cross the bacterium cell membrane is the first step of activity. A discussion in terms of structure-activity relationship is reported.
Es wurden 20 neue Ve&indungen aus Deoxycholdhre spthetisiert Sie enthalten zwei basische Funktionen: an C-24 (Benzylamino. Morpholino, Diethanolamino, N,N-Diethylethylenediiamino, N-Methylpiperazino) und an p-C-3 (Amino, Methylamino, Ethylamino, Benzylamino). AUe Verbindungen weisen interessante mikmbielle Aktiviat auf, ausgedriickt in den nib- gen M.l.C.-Werten (0.9-31 cLg/ml) gegeniiber fhf Gram-positiven und vier Gram-negativen Strtingen. zwei Pilzen und einer Hefe. In einem Fall hemmten die untersuchten Verbindungen die Bildung eines fluoresderenden