Title

Synthesis of Pyranmycin Derivatives with N-1 and O-6 Modifications

Document Type

Article

Journal/Book Title

Bioorganic & Medicinal Chemistry

Publication Date

12-15-2007

Publisher

Elsevier

Volume

15

Issue

24

First Page

7711

Last Page

7719

Abstract

Continuing from our ongoing effort in modifying aminoglycoside antibiotics with the goal of counteracting drug resistant bacteria, we have further derivatized pyranmycin, a neomycin class aminoglycoside antibiotic, with modifications at O-6 and N-1 positions. The revealed SAR results demonstrated that the antibacterial activity of pyranmycin can be modulated by different acylic substituents at O-6. Among these results, the 6-O-aminoethyl derivative, JT050, showed effective activity against resistant strain Escherichia coli (pTZ19U-3) and E. coli (pSF815), which provides insight into further structural modifications.

Comments

PubMed PMID: 17870543; PubMed Central PMCID: PMC2692305

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