In vivo effective dibenzo b,d furan-1-yl-thiazoles as novel PDE-4 inhibitors.
Author | |
---|---|
Abstract | :
Herein we report the synthesis, PDE-4B and TNF-α 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-α 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. |
Year of Publication | :
2016
|
Journal | :
Bioorganic & medicinal chemistry
|
Volume | :
24
|
Issue | :
22
|
Number of Pages | :
5702-5716
|
Date Published | :
2016
|
ISSN Number | :
0968-0896
|
URL | :
https://linkinghub.elsevier.com/retrieve/pii/S0968-0896(16)30698-8
|
DOI | :
10.1016/j.bmc.2016.09.011
|
Short Title | :
Bioorg Med Chem
|
Download citation |