Drugs and Aditives

Recommended Prerequisites

UC´s: Biochemistry I, II and III. Organic Chemistry, Bioinorganics.

Teaching Methods

- Theoretical (T), using suitable audio-visual methodologies (ex. internet access). Active participation from the students will be strongly encouraged.

- Theoretical-practical (TP), where the students will be asked to search and discuss particular cutting-edge topics, under the teacher´s supervision. Analysis of scientific papers. Exercises solving.

- Clarification of doubts (O).

The students will acquainted with the most updated scientific approaches presently used in the field of drug design and development of additives. Access to specific bibliographic sources will be made available.

Learning Outcomes

Study of compounds potentially useful as drugs or as additives (ex. pharmaceutical, food or cosmetics industries).

State-of-the-art strategies will be presented, both from the biological and molecular point perpectives.

Special atention will be paid to Structure-Activity-Relationships (SAR´s), with a view to better understand the behaviour of this kind of systems at the molecular level - rational design approach. New drug delivery strategies are also studied: controlled delivery and targeting.

The student is expected to acquire skills that will allow him(her) to: (i) identify a "lead" compound and assess its possibilities as a drug or an additive, using several techniques - experimental (biological, biochemical, physico-chemical/spectroscopic) and computational (dedicated programs). (ii) choose and make use of the most appropriate methods for the development of a new pharmacological formulation or an additive.

Work Placement(s)

No

Syllabus

A. Structure–Activity Relationships

1. Drug design

(“lead” compound, SARs and QSARs, “Computer-aided molecular design” (CAMD))

2. Factors Ruling Drug Activity

(Physico-chemical properties. Pharmacokinetics, pharmacodynamics)

B. Chemotherapeutic Agents

1. Antioxidants

(Natural and synthetic. Cardiovascular and anticancer prevention, anti-inflammatory and anti-bacterial activities. Antioxidants and diet)

2. Biogenic Polyamines

(Cell growth and differentiation, antioxidant and anti-inflammatory properties. Polyamines and diet. Polyamine metal complexes)

3. Chemotherapeutic Agents in Clinical Use

(Alkylating and metal-based agents, antimetabolites, alkaloids and antibiotics. Endocrine therapy. Immunotherapy)

4. Resistance Mechanisms

5. Controlled Delivery and Targeting

6. Chemoprevention

C. Additives

1. Food Processing Industry

2. Pharmaceutical Industry

(Excipients. Drug controlled delivery)

3. Other Additives and Supplements.

Head Lecturer(s)

Maria Paula Matos Marques Catarro

Assessment Methods

Assessment
Project: 15.0%
Mini Tests: 25.0%
Exam: 60.0%

Bibliography

“An Introduction to Medicinal Chemistry”, G.L. Patrick, 4th ed, OUP, 2009

“Medicinal Chemistry”, T. Nogrady et al., OUP, 2005

“Drug Delivery – Principles and Applications”, B. Wang et al., Wiley-Interscience, 2005

“Fundamentals of Medicinal Chemistry”, G. Thomas, 1st ed, John Wiley&Sons, 2003

“Drug Design Strategies”, D.J Livingstone, A.M. Davis eds., RSC, 2011

"Polyamine Drug Discovery", P. Woster, R. Casero eds, RSC, 2011

“Polyamines in Cancer: Basic Mechanisms and Clinical Approaches”, K. Nishioka, Springer-Verlag, 1996

“Medicinal Chemistry of Anticancer Drugs”, C. Avendano and J.C. Menendez, Elsevier, 2008

“Cisplatin: Chemistry and Biochemistry of a Leading Anticancer Drug”, B. Lippert ed, Wiley, 2006

“The Anticancer Drugs”, W.B.Pratt et al., 2nd ed., OUP, 1994

“Free Radicals in Biology and Medicine”, B. Halliwell et al., OUP, 1999

"Food Additives", A.L. Branen et al. eds, Marcel Dekker, 2002

“Tecnhology of Reduced Additive Foods”, J. Smith, Blackwell, 200