Year-end Sale % OFF 
Abstract
The structure elucidation and biological activity of novel YM-254890 ( 1) analogues and semi-synthetic derivatives are described. Three natural analogues, YM-254891 ( 2), YM-254892 ( 3), and YM-280193 ( 4), were isolated from the fermentation broth of Chromobacterium sp. QS3666, and two hydrogenated derivatives, YM-385780 ( 5) and YM-385781 ( 6), were synthesized from YM-254890. Their structures were determined by one- and two-dimensional NMR studies and mass spectrometry. Among these compounds, two natural analogues 2– 3 which possessed acyl groups at β-HyLeu-1 and one derivative 6 whose conformation was similar to that of 1 showed comparable Gα q/11 inhibitory activity to that of 1. This indicates that the acyl β-HyLeu residue plays an important role in activity and also that the α,β-unsaturated carbonyl group of the N-MeDha residue is not critical to activity. The other hydrogenated derivative 5 had significantly less activity, which could be attributed to conformational differences.
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.
