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Explain the stages of drug discovery, design, and development

BC5062 Coursework

Starting September 2024, biomedical science students must pass each assessment to pass the modules.

In recent years, medicinal chemistry has undergone a revolutionary change. Rapid advances in the biological sciences have resulted in a much better understanding of how the body functions at the cellular and molecular levels. As a result, most research projects in the pharmaceutical industry or university sector now identify a suitable target in the body and design a drug to interact with that target. Understanding the structure and function of the target and the mechanism by which it interacts with potential drugs is crucial to this approach.

In 2000-word report

1) Please select one of these drugs below, draw the chemical structures, and indicate the binding site/s of your chosen molecules. Select one from these below to do your coursework (available from the recommended textbook);

a) Ace inhibitors

b) Artemisinin and related antimalarial drugs

c) Oxamniquine

d) Thymidylate synthase inhibitors

e) Antidepressant agents

f) Aliskiren.

2) Once you selected a drug (from the list above)

a) Explain the stages of drug discovery, design, and development (only on your chosen drug, one of the above lists and not in general). A minimum of 7 chemical structures are to be drawn using one of the recommended chemistry software (BiviaDraw or ChemDraw).

b) Take 4 PrintScreen using the BIOVIA (Drug Discovery Visualiser) to show that you are able to use the software to look at the

i. Amino acids

ii. Ligand

iii. Binding site

iv. Active site

c) Perform Physical properties on your selected drug using the

https://admetmesh.scbdd.com/service/evaluation/cal website.

A 60% of the total mark is allocated for using the recommended medicinal chemistry software, and the rest (40%) will include the write-up and the recent research on your drug of choice.

You should draw all your chemical structures using one of the recommended chemistry software programs. No marks will be given for hand drawing or pictures.

There are two essential things that you should keep in mind;

1) Harvard style is your reference style. Please make sure that all work is correctly cited and referenced. You need to use at least 8 references. 2) Please try to avoid plagiarism; write in your own words.

BC5062 Coursework Details

The BC5062 coursework is a comprehensive academic assessment designed to enhance students` understanding of key concepts and practical applications within their chosen field of study. It challenges learners to critically analyse theoretical frameworks, apply relevant methodologies, and demonstrate problem-solving skills in addressing real-world scenarios. The coursework typically involves a combination of written assignments, case studies, and project-based tasks that require independent research and critical thinking. Students are expected to present well-structured arguments, supported by evidence and academic references, adhering to the standards of scholarly integrity. Through this process, they develop valuable skills such as time management, effective communication, and the ability to synthesise complex information, all of which are crucial for professional success. The BC5062 coursework aims to cultivate a deeper engagement with the subject matter, fostering intellectual growth and practical expertise.

Example Answer - Do Not Copy

Explain the stages of drug discovery, design, and development

1. Chemical Structures and Binding Sites of ACE Inhibitors

Angiotensin-converting enzyme (ACE) inhibitors are a class of drugs used to treat hypertension, heart failure, and other cardiovascular conditions. They work by inhibiting the enzyme ACE, which is responsible for converting angiotensin I into the potent vasoconstrictor angiotensin II.

• Binding Site:

ACE inhibitors bind to the active site of the ACE enzyme, specifically interacting with its zinc ion through their carboxyl group or phosphinic acid group. This prevents the enzyme from cleaving angiotensin I, reducing angiotensin II levels.

• Key Example:Captopril, the first ACE inhibitor developed, includes a sulfhydryl group that interacts with the zinc ion in the ACE active site.

• Chemical Structure of Captopril:
  (Use ChemDraw to illustrate this structure.)

Other examples include Enalapril, Lisinopril, and Ramipril, each with slightly different structures but similar mechanisms.

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2. Stages of Drug Discovery, Design, and Development for ACE Inhibitors

ACE inhibitors were developed following studies of natural peptides from snake venom that inhibited ACE.

a) Discovery Phase:

• ACE inhibitors were inspired by the venom peptide of the Brazilian pit viper (Bothrops jararaca), which showed strong ACE inhibition.
• Structure-activity relationship (SAR) studies on this peptide led to the development of a small molecule capable of mimicking its effects.