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On the determination of the stereochemistry of semisynthetic natural product analogues using chiroptical spectroscopy: desulfurization of epidithiodioxopiperazine fungal metabolites.
Detailed chiroptical studies reveal the desulfurization of chaetocin to unambiguously proceed with retention of configuration and highlighted inconsistencies in the stereochemical assignment of related molecules in the literature.
Melomorsine, a new dimeric indoline alkaloid from Melodinus morsei
A new dimeric indoline alkaloid, melomorsine , and six known alkaloids, 1,2-dehydroaspidospermidine, rhazidine, 11-hydroxytabersonine, aspidospermidine, geissoschizol, and vincoline have been…
Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).
- Edward J Brnardic, Guosen Ye, B. Lawhorn
- Chemistry, BiologyJournal of medicinal chemistry
- 10 October 2018
A novel series of pyrrolidine sulfonamide transient receptor potential vanilloid-4 (TRPV4) antagonists was developed by modification of a previously reported TRPv4 inhibitor to give an optimized lead compound GSK3395879 that demonstrated the ability to inhibit TRPV 4-mediated pulmonary edema in an in vivo rat model.
Cadopherone and colomitide polyketides from Cadophora wood-rot fungi associated with historic expedition huts in Antarctica.