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Module

CHY3410 : Advanced Medicinal Chemistry

  • Offered for Year: 2022/23
  • Module Leader(s): Dr Celine Cano
  • Lecturer: Professor Akane Kawamura, Dr Ian Hardcastle, 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

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
Scheduled Learning And Teaching ActivitiesLecture401:0040:00PiP lectures or a combination of online short recordings of material on VLE each week if no PiP
Guided Independent StudyAssessment preparation and completion201:0020:00Revision for semester 1 examination
Guided Independent StudyAssessment preparation and completion12:002:00End of semester 1 examination
Guided Independent StudyAssessment preparation and completion201:0020:00Revision for semester 2 examination
Guided Independent StudyAssessment preparation and completion12:002:00End of semester 2 examination
Guided Independent StudyAssessment preparation and completion1116:00116:00Background reading of subject, revision and practice of examination papers and questions
Total200:00
Jointly Taught With
Code Title
CHY8822Drug Metabolism and Toxicology
CHY8823Theory and Practice of Chemotherapy
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 Examination1201A50Semester 1 examination
Written Examination1202A50Semester 2 examination
Exam Pairings
Module Code Module Title Semester Comment
CHY8822Drug Metabolism and Toxicology1N/A
CHY8823Theory and Practice of Chemotherapy2N/A
Assessment Rationale And Relationship

The written examinations will assess the level of knowledge and understanding of all aspects of the module, including student reading.

Reading Lists

Timetable