On June 14, 2012, Rohrig, Ute F.; Majjigapu, Somi Reddy; Grosdidier, Aurelien; Bron, Sylvian; Stroobant, Vincent; Pilotte, Luc; Colau, Didier; Vogel, Pierre; Van den Eynde, Benoit J.; Zoete, Vincent; Michielin, Olivier published an article.Application of 5301-96-2 The title of the article was Rational Design of 4-Aryl-1,2,3-Triazoles for Indoleamine 2,3-Dioxygenase 1 Inhibition. And the article contained the following:
Indoleamine 2,3-dioxygenase 1 (IDO1) is an important therapeutic target for the treatment of diseases such as cancer that involve pathol. immune escape. Starting from the scaffold of our previously discovered IDO1 inhibitor 4-phenyl-1,2,3-triazole, we used computational structure-based methods to design more potent ligands. This approach yielded highly efficient low mol. weight inhibitors, the most active being of nanomolar potency both in an enzymic and in a cellular assay, while showing no cellular toxicity and a high selectivity for IDO1 over tryptophan 2,3-dioxygenase (TDO). A quant. structure-activity relationship based on the electrostatic ligand-protein interactions in the docked binding modes and on the quantum chem. derived charges of the triazole ring demonstrated a good explanatory power for the observed activities. The experimental process involved the reaction of 4-(p-Tolyl)-1H-1,2,3-triazole(cas: 5301-96-2).Application of 5301-96-2
The Article related to aryl triazole preparation indoleamine dioxygenase inhibition sar, Pharmacology: Structure-Activity and other aspects.Application of 5301-96-2
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics