Harrison W VanKoten, Breanna Pence, James R Klinkenberg, Siddhartha Das, Steven E Patterson
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引用次数: 0
Abstract
We reported earlier that oseltamivir (Osm, Tamiflu®), an anti-viral agent, inhibits the attachment of trophozoites to intestinal epithelial cells and cyst production in culture. Osm also disassembles lipid rafts (LRs) and the biogenesis of extracellular vesicles (EVs) by Giardia. In the current study, we synthesized forty-one Osm analogs with the derivatization of oseltamivir phosphate. These compounds were tested on giardial growth, and cyst production. Of these, four analogs, i.e., compounds 3b, 2c, 11i, and 11d, were found to have superior activities against trophozoites and cysts compared to the parent oseltamivir. Investigation of the mechanism(s) of action of these agents are in progress and will be reported in due course.
期刊介绍：
Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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