61335-34-0Relevant academic research and scientific papers
Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties
Serra, Silvia,Moineaux, Laurence,Vancraeynest, Christelle,Masereel, Bernard,Wouters, Johan,Pochet, Lionel,Frédérick, Rapha?l
, p. 96 - 105 (2014/06/10)
With the aim to explore the interest of the thiosemicarbazide scaffold for the inhibition of the indoleamine 2,3-dioxygenase (IDO), a promising therapeutic target for anticancer immunotherapy, a series of 32 phenylthiosemicarbazide derivatives was prepared and their IDO inhibition evaluated. Our study demonstrated that among these derivatives, compound 14 characterized with a 4-cyanophenyl group on the thiosemicarbazide was the more potent IDO inhibitor in this series being endowed with an IC50 of 1.2 μM. The SAR depicted showed that substitution in the 3- and 4-position relative to the phenylthiosemicarbazide are very promising whereas substitution in the 2-position always leads to less potent or inactive derivatives. In fact the study highlighted a novel interesting scaffold for IDO inhibition for further development.
Synthesis and antibacterial activity of thiosemicarbazones
Parekh,Desai
, p. 1072 - 1075 (2007/10/03)
The synthesis of 1-[(2′-hydroxy-4′-isopropoxy-5′- nitrophenyl)-ethanone]-4-(aryl)-3-thiosemicarbazones are carried out by refluxing 4-aryl-3-thiosemicarbazides and 2-hydroxy-4-isopropoxy-5- nitroacetophenone in stoichiometric amounts dissolved in aqueous
