Disclosed are compounds, compositions and methods for systemic and local delivery of biologically active molecules.
本发明涉及用于系统和局部传递生物活性分子的化合物、组合物和方法。
Polyamine derivatives
申请人:Slobodkin Gregory
公开号:US08460696B2
公开(公告)日:2013-06-11
Disclosed are compounds, compositions and methods for systemic and local delivery of biologically active molecules.
本发明涉及用于生物活性分子的全身性和局部性递送的化合物、组合物和方法。
Chemoenzymatic Synthesis of Lysophosphatidylnucleosides
作者:Rosa Chillemi、Domenico Russo、Sebastiano Sciuto
DOI:10.1021/jo971826v
日期:1998.5.1
5'-O-Lysophosphatidylnucleosides [5'-O-(1-O-acyl-sn-glycero-3-phosphoryl)nucleosides] were obtained by a two-step chemoenzymatic synthesis. 5'-O-(sn-Glycero-3-phosphoryl)nucleosides (5'-GPNs) were first prepared from a phosphoramidite of 1,2-O-isopropylidene-sn-glycerol and appropriately protected nucleosides, applying the phosphoramidite methodology on the solid phase or in solution. In a following step, the regioselective acylation at the C-l hydroxyl of the glycerol moiety of 5'-GPNs was achieved by a lipase-catalyzed transacylation with activated fatty acid esters in organic solvent. Some deoxyribo- and ribonucleosides, as well, were converted into the corresponding lysophosphatidyl derivatives utilizing either saturated or unsaturated fatty acid esters with different length alkyl chains. The synthesis was also applied to the preparation of O-(1-O-palmitoyl-sn-glycero-3-phosphoryl) conjugates of Acyclovir and AZT, of potential pharmacological interest.
A facile lipase catalyzed access to fatty acid monoesters of
作者:Diego Colombo、Fiamma Ronchetti、Antonio Scala、Ida M. Taino、Lucio Toma
DOI:10.1016/0957-4166(96)00073-0
日期:1996.3
2-O-beta-D-glucopyranosylglycerol was submitted to acylation using Pseudomonas cepacia lipase as catalyst and 2,2,2-trifluoroethyl esters of various long chain carboxylic acids as acyl carriers. Monoacylation was easily accomplished with preferred formation of the (2S)-1-O-acyl derivatives in reactions showing high regio- and diastereoselectivity. (C) 1996 Elsevier Science Ltd
[EN] POLYAMINE DERIVATIVES<br/>[FR] DÉRIVÉS DE POLYAMINE