NES3405 : Advanced Medicinal Chemistry
- Offered for Year: 2024/25
- Module Leader(s): Dr Celine Cano
- Lecturer: Dr Ian Hardcastle, Professor Mike Waring, Professor Akane Kawamura
- Owning School: Natural and Environmental Sciences
- Teaching Location: Newcastle City Campus
Semesters
Your programme is made up of credits, the total differs on programme to programme.
Semester 1 Credit Value: | 10 |
Semester 2 Credit Value: | 10 |
ECTS Credits: | 10.0 |
European Credit Transfer System |
Aims
To introduce the principles of toxicology and drug metabolism; to understand the chemical basis of drug metabolism and its importance in drug discovery; to equip students with a knowledge and understanding of the mechanism of toxicity of drug molecules and other environmental toxins.
To introduce the basic concepts of the aetiology of cancer and pathogenic disease; to develop the concepts of selective toxicity and resistance; to equip students with an understanding of the principles of chemotherapy of cancer and infectious disease; to provide an understanding of the molecular mechanisms underpinning the action of common anticancer and anti-infective drugs.
Outline Of Syllabus
Pharmacokinetics and Drug Metabolism
Pharmacokinetics
Processes and mechanisms of drug metabolism
Selected case studies in drug metabolism
Toxicology
Principles of Toxicology and toxicokinetics
Critical toxicological issues for drug discovery
Allergens and reactive metabolites;
Ion channels – hERG and acetyl choline signaling;
Carcinogenesis
Basic Principles of Enzymology
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
Introduction to cancer
Cytotoxic chemotherapeutic agents: DNA reactive drugs
Antimetabolites
DNA Ttopoisomerase 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
Introduction and historical overview
Principles of antimicrobial chemotherapy
Antibacterial agents: – Penicillin and related β-lactams
Glycopeptidesglycopeptides, quinolones, oxazolidinones and metronidazole
Antifungal agents: – Polyenes, azoles and other antifungals
Antimalarials
Antiviral chemotherapy:
Acyclovir and maraviroc
Teaching Methods
Teaching Activities
Category | Activity | Number | Length | Student Hours | Comment |
---|---|---|---|---|---|
Guided Independent Study | Assessment preparation and completion | 1 | 2:00 | 2:00 | End of semester 1 examination |
Guided Independent Study | Assessment preparation and completion | 20 | 1:00 | 20:00 | Revision for semester 1 examination |
Guided Independent Study | Assessment preparation and completion | 2 | 1:00 | 2:00 | Formative assessment completion |
Scheduled Learning And Teaching Activities | Lecture | 40 | 1:00 | 40:00 | PiP lectures |
Guided Independent Study | Assessment preparation and completion | 1 | 114:00 | 114:00 | Background reading of subject, revision and practice of examination papers and questions |
Guided Independent Study | Assessment preparation and completion | 1 | 2:00 | 2:00 | End of semester 2 examination |
Guided Independent Study | Assessment preparation and completion | 20 | 1:00 | 20:00 | Revision for semester 2 examination |
Total | 200:00 |
Teaching Rationale And Relationship
Lectures will present relevant, research-focused course material, allowing students to gain a greater appreciation of the research activities undertaken by academic staff. Students will be further encouraged to develop their critical thinking skills to participate in advanced discussions of the primary literature relevant to the topics covered.
Assessment Methods
The format of resits will be determined by the Board of Examiners
Exams
Description | Length | Semester | When Set | Percentage | Comment |
---|---|---|---|---|---|
Written Examination | 120 | 1 | A | 50 | Semester 1 examination |
Written Examination | 120 | 2 | A | 50 | Semester 2 examination |
Formative Assessments
Formative Assessment is an assessment which develops your skills in being assessed, allows for you to receive feedback, and prepares you for being assessed. However, it does not count to your final mark.
Description | Semester | When Set | Comment |
---|---|---|---|
Prob solv exercises | 2 | M | Online Canvas quizzes |
Assessment Rationale And Relationship
The written examinations will assess the level of knowledge and understanding of all aspects of the module, including student reading.
Formative assessment to aid students' understanding during the module.
Reading Lists
Timetable
- Timetable Website: www.ncl.ac.uk/timetable/
- NES3405's Timetable