Dix Andrew V, Meseck Carly M, Lowe Adam J, Mitchell Miguel O
Department of Chemistry, Henson School of Science and Technology, Salisbury University, Salisbury, MD 21801, USA.
Bioorg Med Chem Lett. 2006 May 1;16(9):2522-4. doi: 10.1016/j.bmcl.2006.01.093. Epub 2006 Feb 7.
(-)-Deoxypseudophrynaminol 1 possesses 43-fold greater antibacterial potency than the racemate toward Staphylococcus aureus, indicating that the (-)-enantiomer is the biologically active isomer in this assay. Comparison of the percent growth inhibition by derivatives of 1 indicates that prenylation of N8 and replacement of N1-methyl by methyl carbamate are detrimental to antibacterial potency. (-)-1 is a promising lead structure for the development of the novel hexahydropyrrolo[2,3-b]indole class of antibacterial agents.
（-）-脱氧假蟾蜍胺醇1对金黄色葡萄球菌的抗菌效力比外消旋体高43倍，这表明（-）-对映体是该测定中的生物活性异构体。1的衍生物对生长抑制百分比的比较表明，N8的异戊烯基化和用氨基甲酸甲酯取代N1-甲基对抗菌效力不利。（-）-1是开发新型六氢吡咯并[2,3-b]吲哚类抗菌剂的有前景的先导结构。
