title: Synthesis and evaluation of novel neamine derivatives effectively targeting to RNA.
abstract: Three new derivatives of neamine, 3 (NE), 6 (NEA) and 9 (NEL), were synthesized by connecting arginine or lysine to 5-hydroxyl group of neamine using ethylenediamine as a linker. The binding affinities of these derivatives to A site of 16S RNA and TAR RNA indicate that the modification on 5-hydroxyl of neamine by amino acid can enhance the binding affinity of neamine. Compound 9 (NEL) shows some antibacterial activities. These results demonstrate that modification on 5-hydroxyl group of neamine may provide a promising way for the development of potential candidates effectively targeting to RNAs.
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, PR China.
authors.forename: Yanli
authors.initials: Y
authors.lastname: Xu
authors.forename: Hongwei
authors.initials: H
authors.lastname: Jin
authors.forename: Zhenjun
authors.initials: Z
authors.lastname: Yang
authors.forename: Liangren
authors.initials: L
authors.lastname: Zhang
authors.forename: Qi
authors.initials: Q
authors.lastname: Wang
authors.forename: Manning
authors.initials: M
authors.lastname: Li
authors.forename: Lihe
authors.initials: L
authors.lastname: Zhang