الفهرس 
IntroductionOnly 14 pages are availabe for public view
 |  | from | 143 |  |  |
| | | from | 143 | | |
Abstract
A group of PCDSs have been successfully synthesized by coupling of isoniazide or nicotinic acid hydrazide with different aldehydes to give a group of Schiff bases and then quaternization by different bromomalonyl moieties. Introduction of the malonyl moiety lead to a marked increase in the rate of oxidation of the dihydropyridine and 1,2-dihydroisoquinoline carriers. The in vivo distribution studies revealed that the concentration of the tested carriers decrease gradually with time in the blood, while in the brain a marked increase followed by decrease occurred, and this emphasizes the “lock in” effect of the designed carriers. Screening of the prepared compounds for their antidepressant activity revealed that most compounds showed significant antidepressant activity compared to that of imipramine, with a higher activity in the dihydropyridine carriers compared to their quaternized compounds that may be attributed to the “ lock in” effect.