Medicinal Chemistry

Code:

Q4023

Acronym:

Q4023

Level:

400

Keywords
Classification	Keyword
OFICIAL	Chemistry

Instance: 2017/2018 - 2S

Active?	Yes
Responsible unit:	Department of Chemistry and Biochemistry
Course/CS Responsible:	Master in Chemistry

Cycles of Study/Courses

Acronym	No. of Students	Study Plan	Curricular Years	Credits UCN	Credits ECTS	Contact hours	Total Time
M:BQ	12	Plano de Estudos do MBIOQ_2013-2014	1	-	6	56	162
M:Q	6	Official study plan until 2022/2023	1	-	6	56	162

Teaching language

Suitable for English-speaking students

Objectives

The students must apprehend, and understand, the fundamentals of Medicinal Chemistry, as the field of scientific knowledge that emerges from intersection of Chemistry (especially Organic and Bioorganic Chemistry), Pharmacology and other specific fields related to Health Sciences, aiming at the design, chemical synthesis and development of bioactive molecules with potential interest as therapeutic agents (drugs). The students should, also, gain awareness about the relevance of this particular field of Chemistry beyond Academia, in other words, understand the importance and peculiarities of Medicinal Chemistry as one of the cornerstones of Pharmaceutical Industry. Emphasis will also be given to the application of the  so-called emerging technologies, and on the R&D framework, on Medicinal Chemistry.To this end, besides classes and laboratory practices, the UC program will include Seminars on specific topics given by invited experts. Whenever possible, the program will include a visit to the R&D

Learning outcomes and competences

It is intended to provide students with an overview of the Medicinal Chemistry, particularly the industrial level, showing, whenever deemed appropriate, its interdisciplinary nature. Several case studies that illustrate their relevance in health and the alike areas, will be presented, analyzed and discussed. Emphasis will also be given to the implementation of Medicinal Chemistry in designated emerging technologies, and also in the context of research.
The UC features in the program seminars on specific topics given by experts, internal or external guests..

Working method

Presencial

Program

Medicinal Chemistry – Introduction: drugs, drugs of abuse and medicines; drug classification and nomenclature; IUPAC’s MedChem glossary.

General topics on drug action: drug targets and modes of action; relevance of physico-chemical and stereochemical descriptors; pharmacodynamics and pharmacokinetics – ADME[T] properties (absorption, metabolism, excretion, toxicity); administration routes and dose regimens.

Drug discovery: the origin of the drugs, serendipity and chemical modification. Examples. Rational drug design. Pharmacophore, auxophore, toxicophore and metabophore. Examples .Drug design and development .

Drug development: molecular modification strategies; distinguishing hit, lead and candidate; isosteres and bioisosteres; qualitative and quantitative structure-activity relationships (SAR, QSAR); molecular hybridation and simplification; combinatorial synthesis; prodrugs, hard drugs and soft drugs.Strategies for drug targeting and delivery.

Application of the concepts to case studies on drug  discovery and development for different type of diseases  (structures, methods of synthesis, mechanism of action, structure-activity relationship and metabolism).

Mandatory literature

David A. Williams; Foye's Principles of Medicinal Chemistry-, 7th ed, North American Edition , 2012
Camille G. Wermuth, 3rd Edition, Academic Press, , 2008; The Practice of Medicinal Chemistry
David A. Williams, 7th ed, North American Edition , 2012; Foye's Principles of Medicinal Chemistry-

Teaching methods and learning activities

Theoretical Lectures (2 hours/week) with Power-Point support. The slides will be taken as a support to highlight the key theoretical aspects of the course, and will be made available through the website of the UC. Teacher-students interactivity in class will be fostered through discussion of the topics exposed and resolution of open issues.

The laboratorial practices will be comprehend three units (one related to the drug discovery process, another with the biological application and the third with case studies). Each laboratorial module will be preceded by classes where the contents of each module will be presented, analyzed and discussed.

Evaluation Type

Distributed evaluation with final exam

Assessment Components

designation	Weight (%)
Exame	70,00
Trabalho laboratorial	30,00
Total:	100,00

Calculation formula of final grade

NF = 70% NE + 30% NP

Examinations or Special Assignments

n/a

Internship work/project

n/a

Special assessment (TE, DA, ...)

According FCUP pedagogic rules

Classification improvement

according FCUP pedagogic rules