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Macromolecular Prodrugs. IX. Synthesis of Polymer-Fenoprofen Conjugates

Macromolecular Prodrugs. IX. Synthesis of Polymer-Fenoprofen Conjugates

M Zovko, B Zorc, M Lovrek, B Boneschans

Int J Pharm. 2001 Oct 9;228(1-2):129-38.

PMID: 11576775

Abstract:

Synthesis of several polymer-fenoprofen conjugates is described. Fenoprofen was first chemically modified into benzotriazolide 2 and amino acid amide derivatives: glycine fenoprofenamide (3a) and beta-alanine fenoprofenamide (3b) and their benzotriazolides 6a and 6b. Compounds 2 and 6 readily reacted with polyhydroxy aspartamide-type polymers, i.e. poly[alpha,beta-(N-2-hydroxyethyl-DL-aspartamide)] (PHEA) and poly[alpha,beta-(N-3-hydroxypropyl-DL-aspartamide)] (PHPA) forming conjugates 5, 8a,b and 9a,b, respectively. Conjugate 11 was obtained by partial aminolysis of poly-DL-(2,5-dioxo-1,3-pyrrolidinediyl) (PSI) with 2-aminoethyl fenoprofenamide (3c), followed by total aminolysis with 2-hydroxyethylamine. The synthesised polymer-drug conjugates differed in type of covalent bounding, type and/or length of spacer and drug-loading.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP137629324	Poly (α,β-[N-(3-hydroxypropyl)-DL-aspartamide])		137629-32-4	Price

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