Problem

Solutions For An Introduction to Medicinal Chemistry Chapter 13 Problem 6Q

Step-by-Step Solution

Solution 1

Simplification is a commonly used strategy for the lead compounds that are complex, and arise from sources that are natural. The groups that are essential in a drug are first identified by SAR (Specific Absorption Rate).

The parts that are non-essential are then discarded without any loss in the drug activity. The groups that are not the pharmacophore’s part are considered for removal. This removes the centers that are asymmetric and simplifies the carbon skeleton.

Procaine is a drug used in local anaesthesia under the brand name Novocain. It is primarily used in dentistry, and to reduce the pain caused by penicillin injection intramuscularly. Procaine is an ester and amide linked drug used in local anaesthesia.

The local anesthetics that are linked by an ester bond are hydrolyzed to an alcohol and carboxylic acid in presence of esterases and water. The anesthetics that are linked by an amide bond are found to be more stable in solution. This is the reason that these two groups are not located closely in procaine.

Add your Solution
Textbook Solutions and Answers Search
Solutions For Problems in Chapter 13