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. Pharmacokinetics 1. Pharmacokinetics drug DESIGN drug designAimsAims To improve pharmacokinetic properties of lead compound To optimise chemical and metabolic stability (stomach acids / digestive enzymes / metabolic enzymes) To optimise hydrophilic / hydrophobic balance (solubility in blood / solubility in GIT / solubility through cell membranes / access to CNS / excretion rate) Drugs must be polar - to be soluble in aqueous conditions - to interact with molecular targets Dr
• Quick recovery times after surgery 1.2.9 Introducing chemically susceptible groups N CH 2 C O O MeO OMe H MeO (CH)5O C OMe O CH Me MeO OMe OMe OMe 1.2 Drug stability. ... Trojan horse tactic 1.3.1 Linking a biosynthetic building block 1.3 Drug targeting Non selective alkylating agent Toxic N Cl Cl H 3C Uracil Mustard H N HN O O N Cl Cl.
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