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Module

CHY3109 : Advanced Medicinal Chemistry

  • Offered for Year: 2020/21
  • Module Leader(s): Dr Celine Cano
  • Lecturer: Professor Mike Waring, Professor Akane Kawamura, Professor Bernard Golding, Dr James Knight
  • Practical Supervisor: Dr Zuleykha McMillan
  • Owning School: Natural and Environmental Sciences
  • Teaching Location: Newcastle City Campus
Semesters
Semester 1 Credit Value: 20
Semester 2 Credit Value: 10
ECTS Credits: 15.0

Aims

To introduce the principles of toxicology and drug and toxin metabolism; to equip students with a knowledge and understanding of the mechanism of toxicity of a range of chemicals encountered in the environment and workplace.

To introduce the basic concepts of the aetiology of cancer and pathogenic disease; to impart an understanding of the host-pathogen relationship, and the concepts of selective toxicity and resistance; to equip students with an understanding of the basic principles of chemotherapy of cancer and infectious disease; to provide an understanding of the molecular mechanisms underpinning the action of anticancer and anti-infective drugs.

Outline Of Syllabus

Pharmacokinetics and Drug Metabolism (Professor M Waring)
Principles of pharmacokinetics
Processes and mechanisms of drug metabolism
Selected case studies in drug metabolism

Toxicology (Professor M Waring)
Principles of Toxicology and toxicokinetics
Critical toxicological issues for drug discovery
Allergens and reactive metabolites
Ion channels – hERG and acetyl choline signalling
Carcinogenesis and Oxidative Stress

Basic Principles of Enzymology (Prof A Kawamura)
Overview of the role of amino acid side-chains, metal ions and coenzymes in catalysis
Characteristics of enzymes: stability, substrate specificity, stereospecificity,
catalytic groups, factors affecting catalysis, enzyme kinetics
Overview of selected enzyme mechanisms
Model systems for enzymes (probing proximity effects, solvation, strain), acid-base
and nucleophilic catalysis

Cancer Chemotherapy (Dr C Cano)
Introduction to cancer
Cytotoxic chemotherapeutic agents: DNA reactive drugs, antimetabolites, topoisomerase
inhibitors, mitotic poisons
DNA Repair Enzymes
Antiendocrine drugs
Current approaches to cancer chemotherapy
New therapies: Targeting receptor tyrosine kinase signalling and kinase inhibitors case
studies

Chemotherapy of Infectious Diseases (Professor B Golding)
Introduction and historical overview
Principles of antimicrobial chemotherapy
Antibacterial agents: Penicillin and β-lactams, glycopeptides, quinolones,
oxazolidinones and metronidazole
Antifungal agents: Polyenes, azoles and other antifungals
Antimalarials
Antiviral chemotherapy: acyclovir and maraviroc


Laboratory - (Dr C Cano, Dr Zuleykha McMillan)
Synthesis of a variety of antibacterial and antifungal drugs with further
investigation of their physicochemical properties

Teaching Methods

Module leaders are revising this content in light of the Covid 19 restrictions.
Revised and approved detail information will be available by 17 August.

Assessment Methods

Module leaders are revising this content in light of the Covid 19 restrictions.
Revised and approved detail information will be available by 17 August.

Reading Lists

Timetable