Semi-synthetic water-soluble analogs were synthesized from nocathiacin I through the formation of a versatile intermediate nocathiacin amine 5, and subsequent transformation via reductive amination, acylation or urea formation. Several of the novel analogs displayed much improved aqueous solubility over 1, while retained antibacterial activity. Compound 15 and 16 from the amide series, demonstrated excellent in vitro and in vivo antibacterial activity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2012.10.065 | DOI Listing |
Publication Analysis
Top Keywords
antibacterial activity
12
synthesis antibacterial
4
activity novel
4
novel water-soluble
4
water-soluble nocathiacin
4
nocathiacin analogs
4
analogs semi-synthetic
4
semi-synthetic water-soluble
4
water-soluble analogs
4
analogs synthesized
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!