phrm 82400: exam 1: lecture 1: introduction to medicinal chemistry

what is a drug?

any substance that brings about a change in biologic function through its chemical actions

- most of them are organic molecules

- protein drugs (biologics) are more and more popular

in order to modulate the biological activity of a receptor, what does a drug need to do?

- move to the location where the receptor is present

- bind to its receptor

what determines a drug's activity?

functional group

what is a pharmacophore?

a structural motif in which a drugs that bind to the same target share

what is the structural motif mostly responsible for?

binding to the receptor

what are some examples of drug properties that other parts of the drug still affect?

agonism-antagonism, solubility, membrane crossing, metabolism, etc.

morphine, naloxone, and fentanyl all bind to __________

opioid receptors

what do morphine, naloxone, and fentanyl all contain?

piperdine ring and an aromatic ring para to the nitrogen

__________ of the pharmacophore matters

3D structure

morphine and fentanyl are an __________, but naloxone is an __________

agonist; antagonist

what are the properties in which a drug depends on the chemical constituents of the molecule?

- how tightly a drug interacts with the target

- how soluble a drug is in water

- how well a drug crosses the biological membranes

- how fast a drug is degraded in the body

by modifying the structure, one can __________ the drug properties

change

by examining the structure, one can __________ the drug properties

predict

what is "structure" in terms of the structure-activity relationship?

- size

- ionization

- solubility

- hydrophobicity

- stereochemistry

what is "activity" in terms of the structure-activity relationship?

- membrane permeability

- target binding

- metabolism

- excretion