Synthesis and characterization of pH-sensitive conjugate of isoniazid - methoxypoly(ethylene glycol)-b-poly(L-lysine)

被引：2

作者：

Imramovsky, Ales ^{[1
]}

Grusova, Ludmila ^{[1
]}

Benes, Ludvik ^{[2
,3
]}

Pejchal, Vladimir ^{[1
]}

Sedlak, Milos ^{[1
]}

机构：

[1] Univ Pardubice, Inst Organ Chem & Technol, Pardubice 53210, Czech Republic

[2] Univ Pardubice, Joint Lab Solid State Chem, Pardubice 53210, Czech Republic

[3] Univ Pardubice, Inst Macromol Chem AS CR, Vvi, Pardubice 53210, Czech Republic

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 18期

关键词：

Antituberculotics; Isoniazid; Prodrug; pH-sensitivity; poly(ethylene glycol)-b-poly(L-lysine); ACTIVE MOLECULES; IN-VITRO; POLY(ETHYLENE; PRODRUG; PEG;

D O I：

10.1016/j.bmcl.2012.07.054

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present paper deals with the preparation and characterization of a conjugate of isoniazid (INH) with the block copolymer methoxypoly(ethylene glycol)-b-poly(L-lysine) (mPEG-b-PLL). The structure of the conjugate (mPEG-b-PLL-INH) was verified by means of H-1 NMR, GPC, infrared spectroscopy, elemental analysis and powder X-ray diffraction. The conjugate contains six L-lysine units with five INH molecules, which are attached by means of pH-sensitive amidine bond. Under in vitro conditions, the conjugate is hydrolyzed and isoniazid is released (pH 4; 37 degrees C; t(1/2) approximate to 10 h). (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：5952 / 5955

页数：4

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