Study-Unit Description

Study-Unit Description


CODE PHR4311

 
TITLE Medicinal Chemistry 3

 
UM LEVEL 04 - Years 4, 5 in Modular UG or PG Cert Course

 
MQF LEVEL 6

 
ECTS CREDITS 4

 
DEPARTMENT Pharmacy

 
DESCRIPTION The Discovery, Design and Development, including Structure-Activity Relationships (SAR) and where relevant, the pro-drug approach as an integral part of the drug design process.

Similarity and Complementarity-Based Drug Design; Comparing Molecules: a Central Issue in Drug Discovery; The Molecular Similarity Principle; Subjectivity of the Similarity Concept; What can be Similar in Molecules? 2D-Structure Similarity; Shape Similarity; Surface Physicochemical Similarity; H-Bond Similarity; Absence of Particular Features; Pharmacophore Similarity; Comparing Molecular Characteristics; Terminology: Similarity Attributes.

Relevant Characteristics: What is Important?; Relativity of Relevant Properties; Interpretable Characteristics; Global and Local Characteristics; Maximizing Similarity: Object Alignments; The Psychology of Similarity; Molecular Similarity in Medicinal Chemistry Era; Cheminformatics; Medicinal Chemistry Approaches Based on the Similarity Principle; Chemical Modifications; Bioisosteric Replacements; Molecular Mimicry; Mee-too-ism; Peptidomimetics; Lead-Like and Drug-Like Approaches.

Similarity Searching in Databases: Exact and Substructure Searching; Similarity Searching; Semi-Manual Similarity Searching; Similarity.

The design of drug molecules used in the management of malignant disease.

Evolution of malignancy; the identification of targets that can be modulated by drug molecules to mitigate carcinogenesis.

The analysis of the relationships between structure and activity of the various drug classes in contemporary use for the management of neoplastic disease specifically:

- Intercalating Agents;
- Topoisomerase Inhibitors;
- Alkylating Agents;
- Anti metabolites;
- Hormone based therapies;
- Drugs Acting on Structural Proteins;
- Inhibitors of Signalling Pathways;
- Protein Kinase Inhibitors;
- Proteasome Inhibitors.

Analytical and Toxicological Principles:
- The chemistry of the main drugs of abuse and how these can cause toxic effects;
- Techniques used to determine drugs of abuse and analyse them in biological fluids;
- Application of the knowledge of chemistry and techniques of analysis of drugs of abuse in the clinical setting;
- Tests used to quantify drugs of abuse;
- The chemistry of narrow therapeutic index drugs and how these can cause toxic effects;
- Application of the knowledge of chemistry and techniques of analysis of drugs with a narrow therapeutic index in the clinical setting;
- Tests used to quantify narrow therapeutic index drugs.

Study-Unit Aims:

- To reinforce, extend and integrate the knowledge and understanding of the underlying concepts principles and methods of drug design introduced in PHR2028 and PHR3205;
- Highlight characteristics of different pharmaceutical analysis techniques whilst appreciating the impact of the chemical characteristics of the drug or analyte of interest when it comes to separating the drug or analyte of interest from other components and analysing it;
- To understand the toxic effects of drugs of abuse;
- To provide the student with an overall idea of the most popular analytical techniques used to determine and quantify drugs of abuse;
- To understand the toxic effects of drugs having a narrow therapeutic index;
- To provide the student with an overall idea of the most popular analytical techniques used to determine and quantifiy drugs having a narrow therapeutic index.

Learning Outcomes:

1. Knowledge & Understanding:

By the end of this study unit, the student will be able to:
- Understand the principle of molecular similarity and its role in drug design;
- Appreciate the different existing criteria for establishing molecular similarity;
- Appreciate that different methodologies for assessing molecular similarity are applicable in specific circumstances;
- Correlate structure and Activity in the field on anti-cancer pharmacotherapeutic agents;
- Understand and apply basic principles related to separating drugs from other compounds;
- Compare characteristics for different analytical techniques for drugs of abuse;
- Understand and apply basic principles related to separating drugs with a narrow therapeutic index from other compounds;
- Compare characteristics for different analytical techniques for drugs with a narrow therapeutic index.

2. Skills:

By the end of this study unit, the student will be able to:
- Apply different approaches to establishing molecular similarity based on the requirements of specific drug design projects;
- Choose appropriate and relevant analytical methods for the separation of drugs in relation to their chemical characteristics and their use:
- Plan procedures and processes required in the analysis of drugs of abuse and drugs with a narrow therapeutic index;
- Link techniques of analysis with pharmacokinetic studies and the clinical setting.

Main Texts:

- Lemke TL. Review of organic Functional Groups: Introduction to Medicinal Organic Chemistry. USA:Williams & Wilkins. 1992. ISBN 0-7817-4381-8.
- Foye WO. Principles of Medicinal Chemistry. USA: Lippincott, Williams & Wilkins 2008, ISBN 978-0-7817-6870-5.
- Smith HJ and Williams H. Eds. Introduction to the Principles of Drug Design, UK: Harwood Academic Publishers. 2005. ISBN 90-5702-037-8.
- Adrien Albert. Selective Toxicity: The Physico-Chemical Basis of Therapy. USA: Springer. 1985 ISBN 9870-4122-6020-9.
- Souidijn W. The Role of Medicinal Chemistry in Drug Research, Pharmaceutische Weekblad, Scientific Edition 1991; 13(4): 161-6.
- Burger’s Medicinal Chemistry & Drug Discovery. USA: John Wiley and Sons, ISBN 9780 4712-6694-5.
- Fenton JJ. Toxicology: A case oriented approach, Florida: CRC Press. 2002 ISBN 0-849.-0371-0.
- Moffat AC, OSeelton MD, Widdop B, Watts J. Clarke’s Analysis of Drugs and Poisons, Volume 1, 4th Edition. London: Pharmaceutical Press. 2011 ISBN 978-0-85369-711-4.
- Smith FP Seigel JA. Handbook of Forensic Drug Analysis, Burlington: Elsevier Academic Press. 2005 ISBN 0-12-650641-8.

 
RULES/CONDITIONS Before TAKING THIS UNIT YOU MUST TAKE PHR3250

 
STUDY-UNIT TYPE Lecture and Seminar

 
METHOD OF ASSESSMENT
Assessment Component/s Assessment Due Sept. Asst Session Weighting
Examination (3 Hours) SEM2 Yes 100%

 
LECTURER/S Claire Shoemake
Janis Vella

 

 
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It should be noted that all the information in the description above applies to study-units available during the academic year 2023/4. It may be subject to change in subsequent years.

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