1047-94-5Relevant articles and documents
β-GLUCOCEREBROSIDASE CHAPERONES
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Paragraph 0072, (2013/06/06)
The present application relates to compounds of the Formula (I): which are useful or the treatment of diseases in which the wild type or a mutant form of the enzyme β-glucocerebrosidase is implicated.
Synthesis and anti-proliferative activity in vitro of new 5-(2-amino-3-pyridyl)-2-thioxo-3H-1,3,4-oxadiazole derivatives
Liszkiewicz,Kowalska,Wietrzyk,Opolski
, p. 2846 - 2852 (2007/10/03)
The reaction of 2-aminonicotinic acid hydrazide 1 with carbon disulfide gives 5-(2-amino-3-pyridyl)-2-thioxo-3H-1,3,4-oxadiazole 4 which on treatment with ethyl bromoacetate affords 5-(2-amino-3-pyridyl)-2-ethoxycarbonylthio-1,3,4-oxadiazole 5. Treatment of compound 5 with the appropriate primary and secondary amines provided the corresponding oxadiazole derivatives: alkyl-(cycloalkyl-, aryl)-aminocarbamylmethylthio-6-10 or alkyl-(cycloalkyl-, aryl)-amino-11-16. The reaction of 5 with benzylamine furnishes two products: 5-(2-amino-3-pyridyl)-2-benzylamino-1,3,4-oxadiazole 18 and di (benzylcarbamylmethyl)sulfide 19. Selected compounds are tested for their antiproliferative activity in vitro. One of them 19 reveals cytotoxic activity against the cells of 4 human tumor cell lines applied. The ID50 values are in the range of the international activity criterion for synthetic agents (4 μg/mL).