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Module

CHY2410 : Medicinal Chemistry

  • Offered for Year: 2021/22
  • Module Leader(s): Dr Celine Cano
  • Lecturer: Dr Ian Hardcastle
  • Owning School: Natural and Environmental Sciences
  • Teaching Location: Newcastle City Campus
Semesters
Semester 2 Credit Value: 10
ECTS Credits: 5.0

Aims

To equip students with knowledge and understanding of drug-receptor interactions, enzyme chemistry and the principles of drug design and drug action. To provide students with an understanding of the molecular mechanisms underpinning the action of chosen case study drugs.

Outline Of Syllabus

Principles of Medicinal Chemistry and Enzyme Action

Principles of Medicinal Chemistry - Pharmacokinetics; Lipinski’s rule of five;
Pharmacodynamics; Drug-receptor Interactions
Enzymes - What are enzymes?; How do they work?; Mechanisms of Enzyme Catalysis;
Enzyme inhibition and co-enzyme catalysis
Physicochemical properties of drugs - Ionisation constants; Aqueous solubility;
Fick’s Law of diffusion; Lipophilicity; Partition and Distribution Coefficients
Isosterism and Bioisosterism in Drug Discovery
Case studies – Design of Small Molecule Enzyme Inhibitors

Drug Design

Drug Discovery and SARs
Lead optimisation
Mechanisms of Enzyme Inhibition
Case studies in Drug Discovery
Introduction to Structure-Based Drug Design using CCP4 Molecular Graphics (including
a computing workshop with hands on ligand-bound protein crystal structures)

Teaching Methods

Teaching Activities
Category Activity Number Length Student Hours Comment
Structured Guided LearningLecture materials11:001:00PiP Lecture scheduled LTA, Module introduction
Structured Guided LearningLecture materials180:309:00Pre-recorded module content
Guided Independent StudyAssessment preparation and completion110:0010:00Formative assessment coursework
Guided Independent StudyIndependent study157:0057:00Background reading and research
Guided Independent StudyIndependent study60:303:00Online quizzes
Scheduled Learning And Teaching ActivitiesScheduled on-line contact time71:007:00PiP Seminars scheduled LTA, but reverting to online structured guided learning if no PiP possible.
Scheduled Learning And Teaching ActivitiesScheduled on-line contact time12:002:00PiP computer workshop (ChemDraw, Chimera), scheduled LTA, but reverting to online structured guided
Scheduled Learning And Teaching ActivitiesModule talk111:0011:00Office hours, drop in sessions
Total100:00
Teaching Rationale And Relationship

Module content will be delivered using pre-recorded material and PiP seminars with Q+A, worked examples, case studies, and revision materials. PiP sessions will be interactive to ensure that students actively engage with the subject matter.

Assessment Methods

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

Exams
Description Length Semester When Set Percentage Comment
PC Examination1201A100100% Online Assessment (or 2 x 50% alternative assessments if no PiP exams due to social distancing)
Formative Assessments
Description Semester When Set Comment
Written exercise1MFormative Coursework
Assessment Rationale And Relationship

The online assessment and one formative piece will test the student's knowledge and understanding of both the medicinal and the modelling lecture material.

Study Abroad students 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

Timetable