Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors
Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.
Total synthesis and complete structural assignment of thiocillin i
The total synthesis of the thiopeptide antibiotic, thiocillin I, is described. This work unequivocally defines the full structure (constitution and configuration) of the natural product as 1.
Aulakh, Virender S.,Ciufolini, Marco A.
supporting information; experimental part
p. 5900 - 5904
(2011/06/10)
An improved synthesis of pyridine-thiazole cores of thiopeptide antibiotics
(Figure Presented) The oxidation of 2-methylthiazoles to 2-formylthiazoles simplifies the implementation of the Bagley variant of the Bohlmann-Rahtz reaction as a key step in a concise new route to pyridine cores of thiopeptide antibiotics.
Aulakh, Virender S.,Ciufolini, Marco A.
supporting information; experimental part
p. 5750 - 5753
(2009/12/06)
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