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 |
