Synthesis and antibacterial activity of novel water-soluble nocathiacin analogs |
| |
Authors: | Libo Xu Amy K. Farthing James F. Dropinski Peter T. Meinke Christine McCallum Emily Hickey Kun Liu |
| |
Affiliation: | Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|