Transcription of Topic 7.2 INTRODUCTION TO DRUG DESIGN
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Topic 7.2 INTRODUCTION TO DRUG DESIGN
Topic TO DRUGDESIGNC hapter 11 PatrickContentsContentsPart 1: Sections drug and membrane alkyl Masking or removing polar polar Electronic shielding of / replace susceptible metabolic susceptible metabolic susceptible metabolic chemically susceptible a biosynthetic building drugs to monoclonal gut peripheral regions over drug toxicityDrug DESIGN and developmentDrug DESIGN and development Stages:Stages: 1) Identify target disease 2) Identify drug target 3) Establish testing procedures 4) Find a lead compound 5) Structure Activity Relationships (SAR) 6) Identify a pharmacophore 7) Drug DESIGN - optimising target interactions 8) Drug DESIGN - optimising pharmacokinetic properties 9) Toxicological and safety tests10) Chemical development and production11) Patenting and regulatory affairs12) Clinical trials1.
• Useful for reducing CNS side effects Disadvantage: • May introduce unwanted side effects Antifungal agent with poor solubility - skin infections only Cl Cl C O N H N S Cl Tioconazole Systemic antifungal agent improved blood solubility F F C N OH N N N N N 1.1 Solubility and membrane per Fluconazole meability
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