Abstract
A chemical investigation of the Australian pasture soil-derived Actinomadura sp. S4S-00245B09, supported by chemical, bioactivity and cultivation profiling, yielded a new class of terpenyl-quinolin-4(1H)-ones, goondolinones A and B (1 and 2), featuring an unprecedented fused seven-membered ether. Structures were assigned to 1 and 2 on the basis of detailed spectroscopic analysis, including X-ray analysis of 1, and biosynthetic considerations. Goondolinone A (1) lacks antibacterial or antifungal properties, is noncytotoxic to two human carcinoma cell lines, but exhibits selective inhibition of the motility of heartworm Dirofilaria immitis microfilaria (EC50 5.1 μM) and L4 larvae (EC50 21.4 μM). As a new anthelmintic scaffold, future understanding of the structure activity relationship and mechanism of action of 1 could inform the discovery of new treatments for heartworm and other filarial diseases, capable of safeguarding the health and welfare of companion animals.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
