Elective Course: Applications of Carboxylic Acids and Their Derivatives in Pharmacotherapy 1755-F21-ZF02-J

Lectures
Basic concepts and definitions: anatomical-therapeutic-chemical classification of selected molecules, bioisostery, hydrophilicity and lipophilicity, pH of acids and their derivatives.
Discussion of the spatial structure and chemical nomenclature and in accordance with the anatomical-therapeutic-chemical classification of selected molecules. Derivatives of carboxylic acids by isosteric substitutions of the carboxyl group showing different or opposite pharmacology to the parent carboxylic acids (e.g. baclofen, falcophene and salcophene).
History of the discovery of basic pharmaceuticals such as salicylic acid, aspirin, paracetamol and others.
A summary and comparison of the chemical, physical and biological properties of acids and their derivatives determining their therapeutic and toxicological effects. Analysis of the range of pH values of body fluids (e.g. saliva, blood) and organs (e.g. stomach, intestines) versus bioavailability of chemicals.

Total student workload

1. The workload associated with classes requiring the direct participation of academic teachers is: – participation in lectures: 15 hours. The workload associated with classes requiring the direct participation of academic teachers is 15 hours, which corresponds to 0.6 ECTS points. 2. Student workload balance: – participation in lectures: 15 hours – preparation for classes - 5 hours – preparation for assessment and assessment: 5 hours. The total workload associated with the course is 25 hours, which corresponds to 1 ECTS credit. 3. Student workload balance related to scientific activity conducted at the university: 25 hours, which corresponds to 1 ECTS credit. 4. Student workload balance of a practical nature: Not applicable

Learning outcomes - knowledge

The student knows and understands: W1: Principles of designing new drugs based on specific structural properties W2: Modern synthetic methods used in drug design

Learning outcomes - skills

The student is able to: U1: Select appropriate drug candidates based on the steric profiles of chemical compounds U2: Select appropriate synthetic methods for designing drugs with selected therapeutic properties

Learning outcomes - social competencies

The student is ready for: K1: Continuous professional development

Teaching methods

Lectures: - informative lecture (conventional) - problem lecture with multimedia presentation

Expository teaching methods

- informative (conventional) lecture
- problem-based lecture

Type of course

elective course

Prerequisites

The student should have basic knowledge about the properties of chemical compounds obtained as part of the curriculum of organic chemistry, physical chemistry, analytical chemistry

Course coordinators

Łukasz Fijałkowski
Alicja Nowaczyk

Assessment criteria

Lecture:
Credit on the basis of a written paper constituting a study of a selected topic - W1, W2, U1-U2.
The points obtained are converted into grades according to the following scale:

Percentage of points Grade
92-100% Very good
84-91% Good plus
76-83% Good
68-75% Sufficient plus
60-67% Sufficient
0-59% Fail

Laboratories:
- not applicable
Seminars:
- not applicable

Practical placement

not applicable

Bibliography

Primary literature:
1. Montinari, M. R., S. Minelli and R. De Caterina (2019). "The first 3500 years of aspirin history from its roots–A concise summary." Vascular pharmacology 113: 1-8..
2. Brune, K., Renner, B., & Tiegs, G. (2015). Acetaminophen/paracetamol: a history of errors, failures and false decisions. European Journal of Pain, 19(7), 953-965.
3. Fijałkowski, Ł., M. Skubiszewska, G. Grześk, F. K. Koech and A. Nowaczyk (2022). Acetylsalicylic Acid–Primus Inter Pares in Pharmacology. Molecules 27(23): 8412.
4. Ballatore, C., Huryn, D. M., & Smith III, A. B. (2013). Carboxylic acid (bio) isosteres in drug design. ChemMedChem, 8(3), 385-395.

Supplementary literature:
John McMurry Organic Chemistry, A Tenth Edition, The OpenStax, 2023

Additional information

Additional information (registration calendar, class conductors, localization and schedules of classes), might be available in the USOSweb system:

Description of 1755-F21-ZF02-J in USOSweb