الفهرس 
Development and validation of analytical methods for pharmacokinetic study of some phosphodiesterase IV inhibitors and their analogues
abstractOnly 14 pages are availabe for public view
 |  | from | 250 |  |  |
| | | from | 250 | | |
Abstract
Despite recent progress in chronic obstructive pulmonary disease (COPD) therapy, there{u2019}s still an unmet medical need for more potent and safe therapy. One of the most recently used drugs in COPD is the PDE-4 inhibitor roflumilast (ROF).In the present investigation, fourteen ROF analogues were synthesized and evaluated for their PDE-4B inhibition activity. Furthermore, docking studies were undertaken to gain insight into the possible binding mode of the synthesized compounds. The most potent derivatives were further investigated for their PDE-4B/PDE-4D selectivity to estimate their side effects level. Moreover, further pharmacological screening was done by quantification of intracellular cAMP level and TNF-{uF061} % inhibition for further evaluation of their anti-inflammatory activity.The other objective was to test pharmacokinetic parameters for the most potent synthesized derivatives both in vivo and in vitro studies and compare the results with the reference drug ROF