chapter 1 part 1 introduction to medicinal chemistry

Download Chapter 1 Part 1 Introduction to Medicinal Chemistry

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  • Chapter 1 Part 1Introduction 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 medicine?Drugs, pharmaceuticsMedia distinction

    A compound that interacts with a biological system, and produces a biological response (ideally desired and positive)

  • Good vs. Bad DrugsNo medicine has only benefits or drawbacksMorphineExcellent analgesicAddictive, toleranceRespiratory depressionBarbituratesDepressants, sedatives, anestheticsSurgeryOverdoses fatal (Pearl Harbor)

  • HeroinKnown clinically as DiamorphineOne of the best painkillers1898: on market1903: withdrawn (addictive properties)Today: still used

  • Aspirin400 BC: HippocratesChew bark of willow tree for pain (childbirth and eye infections)Active component of willow bark = salicin

  • CocaineSouth American coca bushPlant used as a stimulant, mystical/religious reasonsIsolated 1880sAnesthetic in dentistryAddiction: FreudUsed for depression; other drug addictionDrug development based on structureProcaine (Novocain)

  • Everyday drugsStill produce a response; many are addictiveCaffeineSugarNicotineAlcoholFood additivesVitaminsHerbs Basil: 50 potential carcinogensCultural aspects

  • Good vs. Bad DrugsDepends on:DosageAlmost anything in excess will be toxicChronic exposure

    Measure of safety of drug = therapeutic index

  • Therapeutic indexMeasure of a drugs beneficial effects at low dose vs. harmful effects at high doseComparison of dose levels which lead to toxic effects to dose levels which lead to maximum therapeutic effectsHigh therapeutic index = large margin of safetyMarijuana = 1000Alcohol = 10Does not take chronic use into account

  • Classification of drugsFour main groups (overlap)1. By pharmacological effectsAnalgesics, anti-asthmatics, antipsychotics, etc.Large and varied assortment of drugsMany mechanisms of action2.By chemical structurePenicillins, steroidsCommon skeletonFunctions may be similar or different

  • Classification of drugs3. By target systemAntihistamines Affect a target system (synthesis, release, receptor)Variety of structures due to large number of stages in system4. By target molecule or site of action on targetVery specific classificationExpect structural similarity and common mechanism Easy to classify compounds too narrowly and miss possible positive side effects (new uses for the compound)ZybanViagra



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