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Synthesis and characterization of pH-sensitive conjugate of isoniazid - methoxypoly(ethylene glycol)-b-poly(L-lysine)
Year: 2012
Type of publication: článek v odborném periodiku
Name of source: Bioorganic & Medicinal Chemistry Letters
Publisher name: Pergamon-Elsevier Science Ltd.
Place: Oxford
Page from-to: 5952-5955
Titles:
Language Name Abstract Keywords
cze Syntéza a charakterizace pH-senzitivních konjugátů isoniazidu - methoxypoly(ethylen glykol)-b-poly(L-lysin) Článek se zabývá přípravou a charakterizací konjugátů isoniazidu (INH) s blokovým kopolymerem methoxypoly(ethylen glykol)-b-poly(L-lysinu) (mPEG-b-PLL). Struktura konjugátu (mPEG-b-PLL-INH) byla verifikována s použitím 1H NMR, GPC, IČ, elementární analýzy a práškové X-ray difrakce. Konjugát obsahuje šest L-lysinových jednotek s pěti INH molekulami, které jsou připojeny pH-sensitivní amidinovou vazbou. Za in vitro podmínek se konjugáty hydrolyzují a isoniazid se uvolní (pH 4; 37 C; t(1/2) ca 10 h). Syntéza; charakterizace; pH-senzitivní konjugáty; isoniazid; methoxypolyethylen; glykol-b-polyL-lysin
eng Synthesis and characterization of pH-sensitive conjugate of isoniazid - methoxypoly(ethylene glycol)-b-poly(L-lysine) 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). ACTIVE MOLECULES; IN-VITRO; POLY(ETHYLENE; PRODRUG; PEG; Antituberculotics; Isoniazid; Prodrug; pH-sensitivity; poly(ethylene glycol)-b-poly(L-lysine)

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