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Module

CHY3410 : Advanced Medicinal Chemistry (Inactive)

  • Inactive for Year: 2021/22
  • Module Leader(s): Professor Mike Waring
  • Owning School: Natural and Environmental Sciences
  • Teaching Location: Newcastle City Campus
Semesters
Semester 1 Credit Value: 10
Semester 2 Credit Value: 10
ECTS Credits: 10.0

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 and oxidative Stress

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 ?-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 StudyAssessment preparation and completion200:5016:40Revision for semester 2 examination
Guided Independent StudyAssessment preparation and completion202:0040:00End of semester 2 examination
Guided Independent StudyAssessment preparation and completion184:4084:40Background reading of subject, revision and practice of examination papers and questions
Scheduled Learning And Teaching ActivitiesLecture401:0040:00Lectures
Guided Independent StudyAssessment preparation and completion200:5016:40Revision for semester 1 formative examination
Guided Independent StudyAssessment preparation and completion12:002:00End of semester 1 formative examination
Total200:00
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 Examination1202A100Semester 2 examination
Formative Assessments
Description Semester When Set Comment
PC Examination1ASemester 1 formative examination
Assessment Rationale And Relationship

The formative exam will assess the level of knowledge and understanding from topics studied in semester 1. This will allow the module team to review and feedback on any topic which may have been problematic.

The written examination will assess the level of knowledge and understanding of all aspects of the module, including student reading. The examination will present students with two questions from each of the four topics, and students have to answer one question per topic.

Reading Lists

Timetable