Poly(2-oxazoline)-Antibiotic Conjugates with Penicillins.

作者: Martin Schmidt , Livia K. Bast , Franziska Lanfer , Lena Richter , Elisabeth Hennes

DOI: 10.1021/ACS.BIOCONJCHEM.7B00424

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摘要: The conjugation of antibiotics with polymers is rarely done, but it might be a promising alternative to low-molecular-weight derivatization. two penicillins penicillin G (PenG) and V (PenV) were attached the end groups different water-soluble poly(2-oxazoline)s (POx) via their carboxylic acid function. This ester group was shown more stable against hydrolysis than β-lactam ring penicillins. conjugates are still antimicrobially active up 20 times penicillinase catalyzed hydrolysis. antibiotic activity Staphylococcus aureus in presence 350 higher compared free antibiotics. Conjugates second antimicrobial function, dodecyltrimethylammonium (DDA–X), at starting PenG PenV POx without DDA–X show high penicillinase. For example, ...

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