Chapter 1 Flashcards
What is medicinal chemistry?
The science that deals with the discovery of new therapeutic chemicals and their development into drugs
What is Paul Ehrlich known for?
Making the drug Atoxyl less toxic by making the toxic Arsenic less available for release into the body -> he created a double bond between two As -> less exposed -> Arsphenamine
What are the key ideas of Paul Ehrlich?
-Chemotherapy: using a chemical molecule as a therapeutic entity
-Therapeutic index: ratio of an effective dose to a toxic dose
-Structure-Activity relationship (SAR): certain parts (functional groups or atoms) of the structure of a drug play a specific role in the activity of that drug
-Pharmacophore: Atoms or functional groups that are essential for making a drug work -> discovered by SAR studies, f.e. Ehrlich discovered that As was essential for the function of Atoxyl
Med Chem Terms:
-Drug action: Physiologic change it confers -> Mechanism of action
-Drug target: Is the target a drug interacts with: Protein, acid, nucleic acid
-Lead compound: First promising compound (often don’t make it to the market -> lacks in Bioavailability or too toxic)
What can be done if a lead compound is toxic?
Discover the Pharmacophore with SAR studies, and use it to make the compound less toxic
So what is Pharmacophore?? the group that makes the drug work? or that makes it toxic??
What are the types of chemical compounds?
Natural - semi-synthetic - synthetic
-Natural compound: f.e. extracted from a plant
-semi-synthetic: take the core and modify the functional groups
-synthetic: compounds: related mechanism to the natural product
What is special about drugs from plants?
-structural complexity -> not able to replicate in the lab
-Ring systems and multiple chiral carbons, many of these compounds have more O, rather than N in synthetic compounds
In which diseases are drugs derived from marines promising?
-Cancer, Inflammation, and infectious diseases
-drugs from marine organisms tend to be very toxic, and most of the natural products come from plants
-often hard to get (f.e. only grow in a small region -> so not sustainable)
What does the term antibiotic mean?
-Compound that comes from microorganisms and kills microorganisms
-e.g. Penicillin
Examples of drugs from animal sources: Extracted
-Insulin, Epinephrine
-Thyroxine, Human growth hormone
-not done anymore bc of safety issues, now through recombinant DNA grown in bacteria
How are synthetic drugs created by companies?
Not necessarily from scratch, build from existing structures that have the potential to bind to biological targets -> Privileged Structures by medicinal chemists
