Pre-class Worksheet: Medicinal Chemistry of Drugs for ADHD treatment
Learning Objectives: (CLO#1, SLO #: 2.2.2.7 & 2.2.2.11)
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Discuss classical stimulants Phenylalkylamines
Understand development of Adderall
Phenylalkylamines, phenylethylamines and phenylisopropylamines, represent the largest
group of classical hallucinogens. Phenylisopropropylamine is the class of stimulant drugs
where several compounds related to Amphetamine were made and used. The
phenylethylamines are the α-desmethyl counterparts of the phenylisopropylamines; as
with the indolealkylamines, the α-methyl group's presence increases the agent’s
lipophilicity and reduces its susceptibility to metabolism by monoamine oxidase (MAO).
As a consequence, the phenylethylamines typically produce effects that are qualitatively
similar to those of their corresponding phenylisopropylamines but typically less potent.
Phenylethylamine counterparts of weak phenylisopropylamines might be inactive.
Literally, hundreds of analogs have been examined in human and animal studies.
Please watch the listed video below to learn the development of Adderall.
https://www.youtube.com/watch?v=MeJRBsghMt8
Please write a response to this question in Canvas: What is the importance of the αmethyl group in the phenylisopropylamine stimulates?
- the α-methyl group's presence increases the agent’s lipophilicity and reduces its
susceptibility to metabolism by monoamine oxidase (MAO).