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. 2004 Aug;124(2):125–137. doi: 10.1085/jgp.200409059

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Copyright © 2004, The Rockefeller University Press

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Figure 3. — Glycine hydrazide (GlyH) CFTR inhibitors. (A) Classes of GlyH-101 analogues prepared for analysis of structure–activity relationships showing sites of modification (brackets). Substitutions to benzaldehyde phenyl rings not shown. (B) Reaction schemes for the synthesis of GlyH-101, 126, 201, and 301. Reagents and conditions (see materials and methods for details): (a) ICH₂COOEt, NaOAc, 95°C; (b) N₂H₄.H₂O, EtOH/reflux; (c) 3,5-di-Br-2,4-di-OH-Ph-CHO, EtOH/reflux; (d) 3,5-di-Br-2,4-di-OH-Ph-COCl, pyridine, 22°C; (e) N₂H₄.H₂O, Pd/C (10%), DMF/reflux; (f) glyoxalic acid, 10°C; (g) Na₂BH₃CN/CH₃CN, 48 h; dry HCl, EtOH. (C) Structure (left) and apical Cl⁻ current analysis (right, done as in Fig. 1 C) of OxaH-110 in FRT cells.

	
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