On January 20, 2018, Liessi, Nara; Cichero, Elena; Pesce, Emanuela; Arkel, Maria; Salis, Annalisa; Tomati, Valeria; Paccagnella, Matteo; Damonte, Gianluca; Tasso, Bruno; Galietta, Luis J. V.; Pedemonte, Nicoletta; Fossa, Paola; Millo, Enrico published an article.Application In Synthesis of 2-Amino-4-(4-iodophenyl)thiazole The title of the article was Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools. And the article contained the following:
The most common CF mutation, F508del, impairs the processing and gating of CFTR protein. This deletion results in the improper folding of the protein and its degradation before it reaches the plasma membrane of epithelial cells. Present correctors, like VX809 only induce a partial rescue of the mutant protein. Our previous studies reported a class of compounds, called aminoarylthiazoles (AATs), featuring an interesting activity as correctors. Some of them show additive effect with VX-809 (I) indicating a different mechanism of action. In an attempt to construct more interesting mols., it was thought to generate chem. hybrid compounds, blending a portion of VX-809 merged to the thiazole scaffold. This approach was guided by the development of QSAR analyses, which were performed based on the F508del correctors so far disclosed in the literature. This strategy was aimed at exploring the key requirements turning in the corrector ability of the collected derivatives and allowed us to derive a predictive model guiding for the synthesis of novel hybrids as promising correctors. The new mols. were tested in functional and biochem. assays on bronchial CFBE41o-cells expressing F508del-CFTR showing a promising corrector activity. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).Application In Synthesis of 2-Amino-4-(4-iodophenyl)thiazole
The Article related to thiazole vx809 hybrid cystic fibrosis deletion mutation corrector qsar, aminoarylthiazole, cftr, corrector, cystic fibrosis, qsar, vx809, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Application In Synthesis of 2-Amino-4-(4-iodophenyl)thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica