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

DOI

10.1016/j.bmc.2007.08.059

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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