- Discovery and efficient synthesis of a biologically active alkaloid inspired by thiostrepton biosynthesis
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Thiostrepton, a natural peptide macrocycle, is of great interest due to its structural complexity and numerous biological activities, including anti-bacterial, anti-tumor, and anti-plasmodial activities. The quinaldic acid (QA) moiety-containing side ring (loop 2) was proven to play an important role in carrying out these functions. Previously, we proposed biosynthetic logic for thiostrepton loop 2 and demonstrated the formation mechanism of QA. Herein, we report the discovery and efficient synthesis of a biologically active alkaloid, that is, a key intermediate involved in the thiostrepton biosynthetic pathway. A chemo-enzymatic method was performed to synthesize the molecule, and a series of analogs were prepared for bioassays, which included the examination of anti-bacterial and anti-tumor activities.
- Zheng, Qingfei,Wang, Shoufeng,Liu, Wen
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p. 7686 - 7690
(2014/12/10)
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- CETP INHIBITORS AND METABOLITES THEREOF
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Compounds resulting from the administration of torcetrapib to a mammal, and the use of such compounds as an indicator or biomarker to the presence or exposure of torcetrapib in the plasma of a mammal including humans. The invention is also directed to cholesteryl ester transfer protein (CET P) inhibitors, pharmaceutical compositions containing such inhibitors and the usi-, of such inhibitors to elevate cert in plasma lipid levels, including high den~;ity lipoprotein (HDL)-cholesterol and t lower certain other plasma lipid levels, such as low density lipoprotein (LDL)-chole terol and triglycerides.
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Page/Page column 32-33
(2010/02/11)
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