Bellini A M, Mencini E, Quaglio M P, Guarneri M, Fini A
Dipartimento di Scienze Farmaceutiche, Ferrara, Italy.
Arch Pharm (Weinheim). 1990 Apr;323(4):201-5. doi: 10.1002/ardp.19903230404.
Twenty new compounds derived from deoxycholic acid have been synthesized. They contain two basic functions: at C-24 (benzylamino, morpholino, diethanolamino, N,N-diethylethylenediamino, N-methylpiperazino) and at beta-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-micrograms/ml) against five Gram(+) and four Gram(-) strains, two fungi and one yeast. The compounds inhibit the production of a fluorescent pigment in Pseudomonas 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.
已合成了20种源自脱氧胆酸的新化合物。它们含有两种基本官能团：在C-24位（苄氨基、吗啉基、二乙醇氨基、N,N-二乙基乙二胺基、N-甲基哌嗪基）和在β-C-3位（氨基、甲氨基、乙氨基、苄氨基）。这些化合物表现出有趣的抗菌活性，以对5种革兰氏阳性菌和4种革兰氏阴性菌、2种真菌和1种酵母的低最低抑菌浓度（M.I.C.值为0.9 - 31微克/毫升）来表示。这些化合物抑制铜绿假单胞菌中荧光色素的产生：这一结果表明穿过细菌细胞膜的能力是活性的第一步。报道了关于构效关系的讨论。
