- Perform Structure Activity Identification Sar Of Alpidem That Has The Estructure As In The Example With Other Drug I 1 (3.9 KiB) Viewed 66 times
- Perform Structure Activity Identification Sar Of Alpidem That Has The Estructure As In The Example With Other Drug I 2 (41.67 KiB) Viewed 66 times
SAR:- R₂ A FIZ B C P₂ -R₂ 1. In ring A an electron withdrawing group such as Cl, Br, No,,or CF3,CN at position 7. 2. A methyl group is attached to the nitrogen atom in 1 position in ring B. however substituents at position 1that are metabolically removed are still clinically useful. ex:-flurazepam,prazepam. 3. Replacement of the carbonyl function with two hydrogens in the second positiion gives medazepam less potent than diazepam. Replacement of one of the hydrogen with a OH on third position lowers activity on the one hand and aids elimination on the other. 4. Introduction of a carboxyl function in the third position increases the duration of action (clorazepate) and also favours formation of a water soluble salts.