title: Click-based synthesis of triazolobithiazole ΔF508-CFTR correctors for cystic fibrosis.
abstract: Copper catalyzed azide-alkyne cycloaddition (CuAAC) chemistry is reported for the construction of previously unknown 5-(1H-1,2,3-triazol-1-yl)-4,5'-bithiazoles from 2-bromo-1-(thiazol-5-yl)ethanones. These novel triazolobithiazoles are shown to have cystic fibrosis (CF) corrector activity and, compared to the benchmark bithiazole CF corrector corr-4a, improved logP values (4.5 vs 5.96).
authors: Department of Chemistry, University of California, Davis, CA 95616, USA.
authors: Michael B
authors: MB
authors: Donald
authors: Kevin X
authors: KX
authors: Rodriguez
authors: Hannah
authors: H
authors: Shay
authors: Puay-Wah
authors: PW
authors: Phuan
authors: A S
authors: AS
authors: Verkman
authors: Mark J
authors: MJ
authors: Kurth
mesh_terms: D003550:Cystic Fibrosis / Q000188:drug therapy*; D019005:Cystic Fibrosis Transmembrane Conductance Regulator / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D013844:Thiazoles; D014230:Triazoles; C093349:cystic fibrosis transmembrane conductance regulator delta F508; D019005:Cystic Fibrosis Transmembrane Conductance Regulator