Optimization of substituted imidazobenzodiazepines as novel asthma treatments

Volume: 126, Pages: 550 - 560
Published: Jan 1, 2017
Abstract
We describe the synthesis of analogs of XHE-III-74, a selective α4β3γ2 GABAAR ligand, shown to relax airway smooth muscle ex vivo and reduce airway hyperresponsiveness in a murine asthma model. To improve properties of this compound as an asthma therapeutic, a series of analogs with a deuterated methoxy group in place of methoxy group at C-8 position was evaluated for isotope effects in preclinical assays; including microsomal stability,...
Paper Details
Title
Optimization of substituted imidazobenzodiazepines as novel asthma treatments
Published Date
Jan 1, 2017
Volume
126
Pages
550 - 560
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