Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 24, Issue 22, Pages 5702-5716Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.09.011
Keywords
PDE-4 inhibitors; TNF-alpha; Dibenzofuran
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Herein we report the synthesis, PDE-4B and TNF-alpha inhibitory activities of a few dibenzo[b,d]furan-1-yl-thiazole derivatives. The hydroxycyclohexanol amide derivatives 14, 18, 24, 29, 31 and 33 exhibited promising in vitro PDE-4B and TNF-alpha inhibitory activities. Compound 24 showed good systemic availability in preclinical animal models and was also found to be non-toxic (exploratory mutagenicity test). Further it exhibited promising results in in vivo asthma/COPD and Uveitis models. (C) 2016 Elsevier Ltd. All rights reserved.
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