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EnglishThe phenylhydrazone RDR-1 is endowed with moderate activity as F508del-CFTR corrector; nevertheless, its simple structure enables stimulating developments in this class of correctors. Therefore, we synthesized a number of phenylhydrazones 3 by reacting phenylhydrazine derivatives 1 with furfural derivatives 2. By the same reaction, also the pyridine derivatives 4, the thiophene derivatives 5, and the hydrazides 6 and 7 were prepared. All compounds were tested as F508del-CFTR correctors in the cystic fibrosis (CF) bronchial epithelial cell line CFBE41o-, using corr-4a and VX-809 as controls. Some of the tested compounds emerged as interesting F508del-CFTR correctors at 20 μM (3c) and 2 μM (5d). 3c and 5d administered together with VX-809 produced a satisfactory additivity of action. When the structure of 5d was overlapped with RDR-1 and five other established correctors, a shared central design was clearly visible. This fact may be of interest in the search for new F508del-CFTR correctors. Starting from RDR-1, a known F508del-CFTR corrector, some phenylhydrazones were synthesized. Two new compounds (3c and 5d) showed encouraging activity and, when administered together with the corrector VX-809, gave an additivity of action. Overlapping the molecular design of 5d with RDR-1 and other known correctors revealed a common structural moiety, which may help in the search for new drugs against cystic fibrosis.
Phenylhydrazones as Correctors of a Mutant Cystic Fibrosis Transmembrane Conductance Regulator / Nieddu, Erika; Pollarolo, Benedetta; Mazzei, Marco T.; Anzaldi, Maria; Schenone, Silvia; Pedemonte, Nicoletta; Galietta, Luis J. V.; Mazzei, Mauro. - STAMPA. - 349(2016), pp. 112-123.
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| Titolo: | Phenylhydrazones as Correctors of a Mutant Cystic Fibrosis Transmembrane Conductance Regulator |
| Autori: | |
| Data di pubblicazione: | 2016 |
| Rivista: | |
| Citazione: | Phenylhydrazones as Correctors of a Mutant Cystic Fibrosis Transmembrane Conductance Regulator / Nieddu, Erika; Pollarolo, Benedetta; Mazzei, Marco T.; Anzaldi, Maria; Schenone, Silvia; Pedemonte, Nicoletta; Galietta, Luis J. V.; Mazzei, Mauro. - STAMPA. - 349(2016), pp. 112-123. |
| Handle: | http://hdl.handle.net/11567/842753 |
| Appare nelle tipologie: | 01.01 - Articolo su rivista |
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