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Introduction to Medicinal Chemistry

What is medicinal chemistry?. The science that deals with the discovery or design of new therapeutic chemicals and the development of these chemicals into useful medicine. What is

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Introduction to Medicinal Chemistry

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    1. Introduction to Medicinal Chemistry Chapter 1

    2. What is medicinal chemistry? The science that deals with the discovery or design of new therapeutic chemicals and the development of these chemicals into useful medicine

    3. What is “medicine”? Drugs, pharmaceutics Media distinction A compound that interacts with a biological system, and produces a biological response (ideally desired and positive)

    4. “Good” vs. “Bad” Drugs No medicine has only benefits or drawbacks Morphine Excellent analgesic Addictive, tolerance Respiratory depression Barbiturates Depressants, sedatives, anesthetics Surgery Overdoses fatal (Pearl Harbor)

    5. Heroin Diamorphine One of the best painkillers (“hero”) 1898: on market 1903: withdrawn (addictive properties) Today: still used

    6. Everyday drugs Still produce a response; many are addictive Caffeine Sugar Nicotine Alcohol Food additives Vitamins Herbs Basil: 50 potential carcinogens Cultural aspects

    7. “Good” vs. “Bad” Drugs Depends on: Dosage Almost anything in excess will be toxic Chronic exposure Measure of safety of drug = therapeutic index

    8. Therapeutic index Measure of a drug’s beneficial effects at low dose vs. harmful effects at high dose Comparison of dose levels which lead to toxic effects to dose levels which lead to maximum therapeutic effects High therapeutic index = large margin of safety Marijuana = 1000 Alcohol = 10 Does not take chronic use into account

    9. Medicinal Chemistry Under what conditions are drugs “good,” and what do they do to the body? Curare/Tubocurarine

    10. Classification of drugs Four main groups (overlap) 1. By biological effect Analgesics, anti-asthmatics, antipsychotics, etc. Large and varied assortment of drugs Many mechanisms of action 2. By chemical structure Penicillins, opiates Common skeleton Functions similar or different

    11. Classification of drugs 3. By target system Antihistamines Affect a target system (synthesis, release, receptor) Variety of structures due to large number of stages in system 4. By target site of action Anticholinesterases (inhibit acetylcholinesterase in CNS) Target enzyme or receptor Usually common mechanism

    12. Controlled Substances Act Drug scheduling (I – V) Potential for abuse, safety, dependence Currently accepted for medical use DEA list of scheduled drugs

    13. History of Medicinal Chemistry Studied/practiced for thousands of years Medicine men/witch doctors Roots, plants, trees, berries, herbs Often placebos Leeches and maggots Last 150 years: Mechanism of reaction/response 1909: first chemotherapy (Ehrlich) Salvarsan (compound “606”) for syphilis Aside: naming drugs (see App.6) Later replaced with penicillin (1940s) 2005: Structure determination

    14. Aspirin 400 BC: Hippocrates Chew bark of willow tree for pain (childbirth and eye infections) Active component of willow bark = salicin

    15. Cocaine South American coca bush Plant used as a stimulant, mystical/religious reasons Isolated 1880’s Anesthetic in dentistry Addiction: Freud Used for depression; other drug addiction Drug development based on structure Procaine (Novocain)

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