Q$4$: Medical Chemistry

Benzodiazepine $-$Structure$-$Activity Relationship $($SAR$)$

Use the $7$ analogues listed below:

Diazepam

Flurazepam

Lorazepam

Alprazolam

Clonazepam

Temazepam

Oxazepam

$1.$ What is the original structure this analogue was derived from? $($parent$)$

$2.$ What were the limitations of the original structure?

$-$ What was the problem pharmacokinetic, pharmacodynamic, toxicological, or something else? $($use the structure to explain$).$

$3.$ What structure$/$functional group was adjusted, removed, replaced, or added? How did that affect the performance of the drug? $**$i have circled in red$**$

$4.$ What structure remained and how did that affect the performance of the drug? $**$i have circled in red$**$

$5.$ What is the need for $7$ different analogues? $-$ list reason$($s$)$ for all $7$

I have provided an original structure of Benzodiazepine and the $7$ analogues mentioned.

Please use those structures and numbering to explain.

Example: Why was Cl added at position $7$ of ring A in Diazepam? $($and why did it remain in following analogues$)$