Global Opportunities

CHY3109 : Advanced Medicinal Chemistry (Inactive)

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
Principles of 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 signalling
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
Overview of selected enzyme mechanisms
Model systems for enzymes (probing proximity effects, solvation, strain), acid-base
and nucleophilic catalysis

Cancer Chemotherapy
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
Introduction and historical overview
Principles of antimicrobial chemotherapy
Antibacterial agents: ?-lactam antibiotics, glycopeptides, quinolones,
oxazolidinones, macrolides
Antifungal agents: polyene macrolides, azoles, allylamines
Antiprotozoal agents (antimalarials: quinine and synthetic analogues, artemisinin; metronidazole)
Antiviral chemotherapy: drugs against Covid-19, neuraminidase inhibitors (influenza), chain terminators (e.g. acyclovir), drugs for HIV (reverse transcriptase and protease inhibitors)


Laboratory
Synthesis of a variety of antibacterial and antifungal drugs with further
investigation of their physicochemical properties

Teaching Methods

Teaching Activities
Category Activity Number Length Student Hours Comment
Structured Guided LearningLecture materials200:3010:00PiP lectures or a combination of online short recordings of material on VLE each week if no PiP
Guided Independent StudyAssessment preparation and completion115:0015:00Alternative online assessment of semester 1
Guided Independent StudyAssessment preparation and completion141:0014:00Revision for semester 1 assessment
Guided Independent StudyAssessment preparation and completion141:0014:00Alternative online assessment semester 2
Guided Independent StudyAssessment preparation and completion141:0014:00Revision for semester 2 assessment
Guided Independent StudyAssessment preparation and completion120:0020:00Laboratory online assessment
Guided Independent StudyAssessment preparation and completion112:0012:00Laboratory Skills assessment
Scheduled Learning And Teaching ActivitiesPractical510:0050:00PiP laboratory sessions.
Guided Independent StudyDirected research and reading161:0061:00Reading materials related to module topics
Scheduled Learning And Teaching ActivitiesDrop-in/surgery80:304:00Online email support
Scheduled Learning And Teaching ActivitiesDrop-in/surgery221:0022:00Office hour drop ins
Guided Independent StudyIndependent study160:0060:00Independent study, background reading around all topics within the module
Scheduled Learning And Teaching ActivitiesModule talk80:304:00Overview and discussion within topics
Total300:00
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 online 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

Exams
Description Length Semester When Set Percentage Comment
Written Examination1201A33Exam or online assessment in the event of no PiP exams due to social distancing.
Written Examination1202A34Exam or online assessment in the event of no PiP exams due to social distancing.
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 report1M33Laboratory online assessment
Zero Weighted Pass/Fail Assessments
Description When Set Comment
Practical/lab reportMLaboratory Skills Assessment
Assessment Rationale And Relationship

The alternate online assessment will assess the student's knowledge and understanding of the basic principles of the subject as well as the 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.

Students are required to obtain at least 35% in the laboratory component in order for the examination mark to be included in the final module mark. Students who score <35% in the laboratory will obtain a module mark based solely on the laboratory practical.

Study Abroad students may request to take their assessment 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

Timetable