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CHY3109 : Advanced Medicinal Chemistry

  • Offered for Year: 2019/20
  • Module Leader(s): Dr Celine Cano
  • Lecturer: Professor Mike Waring, Dr James Knight, Professor Bernard Golding
  • Practical Supervisor: Dr Zuleykha McMillan
  • Owning School: Natural and Environmental Sciences
  • Teaching Location: Newcastle City Campus
Semester 1 Credit Value: 20
Semester 2 Credit Value: 10
ECTS Credits: 15.0


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
Drug metabolism as applied to diabetes drugs

Toxicology (Professor M Waring)

Principles of Toxicology
Allergens and reactive metabolites
Oxidative Stress
Ion channels – hERG and acetyl choline signaling

Basic Principles of Enzymology (Dr J Knight)

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
Model systems for enzymes (probing proximity effects, solvation, strain), acid-base and nucleophilic catalysis
Overview of selected enzyme mechanisms including those with no cofactor/metal (e.g. glutathione transferases)
Redox cofactors
Small molecule activation by non-metallic cofactors
Radical enzymes

Cancer Chemotherapy (Dr C Cano)

Introduction to cancer
DNA reactive drugs
DNA Topoisomerase inhibitors
Mitotic poisons
DNA Repair Enzymes
Antiendocrine drugs
Current approaches to cancer chemotherapy
New therapies: Targeting receptor tyrosine kinase signalling
Kinase inhibitors case studies

Chemotherapy of Infectious Diseases (Professor B Golding)

Introduction and historical overview
Principles of antimicrobial chemotherapy
Antibacterial agents – Penicillin and related B-lactam
Antibacterial agents – Glycopeptides, quinolones, and oxazolidinones
Antifungal agents – Polyenes and azoles
Antifungal agents – Azoles and other antifungals
Malaria and its treatment
Antiviral chemotherapy
Acyclovir and maraviroc

Laboratory - (Dr C Cano, Dr Zuleykha McMillan)
Experiment 1. Synthesis of chalcone derivatives
Experiment 2. Synthesis of penicillin derivatives
Experiment 3. The Baker-Venkataraman Synthesis of Flavones
Experiment 4. Biological assay and physical properties of drugs

Teaching Methods

Teaching Activities
Category Activity Number Length Student Hours Comment
Guided Independent StudyAssessment preparation and completion55:0025:00Writing practical reports
Guided Independent StudyAssessment preparation and completion200:5016:40Revision for semester 2 examination
Guided Independent StudyAssessment preparation and completion200:5016:40Revision for semester 1 examination
Guided Independent StudyAssessment preparation and completion12:002:00End of semester 2 examination
Guided Independent StudyAssessment preparation and completion12:002:00End of semester 1 examination
Scheduled Learning And Teaching ActivitiesLecture401:0040:00N/A
Scheduled Learning And Teaching ActivitiesPractical59:0045:005x9h Practical sessions take place over 5 weeks
Guided Independent StudyIndependent study1152:40152:40Background reading and practice past paper examination questions
Jointly Taught With
Code Title
CHY8822Drug Metabolism and Toxicology
CHY8823Theory and Practice of Chemotherapy
CHY3110Advanced Medicinal Chemistry
Teaching Rationale And Relationship

Students acquire an understanding of the subject through attendance and participation in lectures. An understanding of the topics is reinforced by problem solving, and critical background reading of the scientific literature.

In practical classes competencies in practical procedures, observation, record-keeping and report writing, will be taught and learnt.

Assessment Methods

The format of resits will be determined by the Board of Examiners

Description Length Semester When Set Percentage Comment
Written Examination1201A34N/A
Written Examination1202A33N/A
Exam Pairings
Module Code Module Title Semester Comment
CHY8822Drug Metabolism and Toxicology1N/A
CHY8823Theory and Practice of Chemotherapy2N/A
CHY3110Advanced Medicinal Chemistry1N/A
Other Assessment
Description Semester When Set Percentage Comment
Practical/lab report1M33composed of several individual laboratory reports as specified in the practical course handbook
Assessment Rationale And Relationship

The examinations will assess the student's knowledge and understanding of the basic principles of the subject. The coursework will assess information literacy in the context of chemical toxicology and written presentation skills.

The laboratory component practical involves the assessment of a diverse selection of skills learnt in about 4 experiments per student, spread over the major areas of medicinal chemistry.

Study Abroad students may request to take their exam before the semester 1 exam period, in which case the format of the paper may differ from that shown in the MOF. Study Abroad students should contact the school to discuss this.

Reading Lists