Libraries of C-5 Substituted Imidazoles and Oxazoles by Sequential Van Leusen (VL)–Suzuki, VL–Heck and VL–Sonogashira in Imidazolium-ILs with Piperidine-Appended-IL as Base
Facile access to diverse C5-substituted imidazoles and oxazoles via sequential Van Leusen–Suzuki, Van Leusen–Heck, and Van Leusen–Sonogashira protocols, employing imidazolium-ILs as solvents along with piperidine-appended imidazolium [PAIM][NTf2/sub
Savanur, Hemantkumar M.,Kalkhambkar, Rajesh G.,Laali, Kenneth K.
supporting information
p. 5285 - 5288
(2018/09/06)
Discovery of biaryl inhibitors of H+/K+ ATPase
We report the identification of a novel biaryl template for H+/K+ ATPase inhibition. Evaluation of critical SAR features within the biaryl imidazole framework and the use of pharmacophore modelling against known imidazopyridine and azaindole templates suggested that the geometry of the molecule is key to achieving activity. Herein we present our work optimising the potency of the molecule through modifications and substitutions to each of the ring systems. In particular sub-micromolar potency is achieved with (4b) presumably through a proposed intramolecular hydrogen bond that ensures the required imidazole basic centre is appropriately located.
Garton, Neil,Bailey, Nick,Bamford, Mark,Demont, Emmanuel,Farre-Gutierrez, Irene,Hutley, Gail,Bravi, Gianpaolo,Pickering, Paula
scheme or table
p. 1049 - 1054
(2010/06/12)
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