Biodiversity in Drug Discovery

Code:

QF13002

Acronym:

BDF

Keywords
Classification	Keyword
CNAEF	Life sciences

Instance: 2021/2022 - 1S

Active?	Yes
Responsible unit:	Organic and Pharmaceutical Chemistry Laboratory
Course/CS Responsible:	MSc in Pharmaceutical Chemistry

Cycles of Study/Courses

Acronym	No. of Students	Study Plan	Curricular Years	Credits UCN	Credits ECTS	Contact hours	Total Time
MQF	22	Official Curriculum	1	-	6	50	162

Teaching language

Suitable for English-speaking students

Objectives

It is intended that students acquire a set of knowledge essential to follow the evolution that has been the application of the Natural Products in Medicinal Chemistry, especially in the search of new drugs, including the use as models for development, semi-synthesis and total synthesis of bioactive compounds, as well as important tools for investigating novel mechanisms of action or discovery of new receptors. Another objective is to present technologies based on the genetic manipulation of biosynthetic enzymes of natural products, particularly in combinatorial biosynthesis, as well as other strategies used to obtain biodiversity.

Learning outcomes and competences

Students will be able to monitor the progress that has been the application of natural products of marine and terrestrial origin including plants, algae and microorganisms (bacteria and fungi of terrestrial and marine origin) in drug discovery. Will also be able to recognize the more recent approaches that allow obtaining biodiversity, including in particular the synthesis of libraries inspired by natural products.

Working method

Presencial

Program

- Introduction.

- Biodiversity "macro" (plants and marine organisms) and "micro" (bacteria and fungi from terrestrial and marine origin)

3 Natural products as drugs or as lead compounds in medicinal chemistry:
- Alkaloids (morphine , nicotine, muscarine , curare , tubocurarine , physostigmine )
- Penicillins and cephalosporins
- Natural anticancer agents: alkylating agents ( mitomycin C ) , intercalating agents ( anthracyclines and actinomycins ) , topoisomerase inhibitors ( camptothecin and podophyllotoxin and derivatives ) , degrading agents ( bleomycins ) , inhibitors of DNA synthesis ( cytarabine ), antimitotic agents ( vinblastine and analogues and taxol analogues)
4 . Methodologies for the isolation, purification of secondary metabolites:
- Bioguided Isolation
- Extraction : maceration , percolation , soxhlet extraction , pressurized solvent extraction , steam distillation, supercritical fluid extraction
- Purification: Chromatographic techniques
5. Structure determination of secondary metabolites: UV- Vis, IR , 1H NMR and 13C NMR , DEPT , COSY , HETCOR , HSQC , HMBC . Case studies .
- Biosynthetic Pathways as a source and model for biodiversity: polyketides, alkaloids, secondary metabolites derived from mevalonate and shimimate.

 

The classes will be dedicated to the elaboration, presentation and discussion of oral communications, which include case studies related to the program content discussed in the lectures.

Mandatory literature

The Royal Society of Chemistry, Thomas Graham House, Science Park, Cambridge, United Kingdom; Natural Product Chemistry for Drug Discovery, Antony D Buss, Mark S Butler, 2010
Gordon M. Cragg, David J. Newman; Biodiversity: A Continuing Source Of Novel Drug Leads, Pure Appl. Chem. 77(1), 7-24., 2005

Complementary Bibliography

Beal J. L. 340; Natural products as medicinal agents. ISBN: 3-7773-0540-5
Dermarderosian Ara 340; The^review of natural products. ISBN: 1-57439-141-0
Patrick Graham L.; An^introduction to medicinal chemistry. ISBN: 0 19 850533 7
Avendano Carmen; Medicinal chemistry of anticancer drugs. ISBN: 978-0-444-52824-7

Teaching methods and learning activities

Lectures, using power-point presentations, will correspond to explanations and will promote discussion and interaction with students, as well as the interrelation of knowledge and critical thinking of students. An oral communication on a provided theme will be presented and performed by the students .

keywords

Health sciences
Natural sciences > Biological sciences > Biodiversity
Physical sciences > Chemistry > Organic chemistry

Evaluation Type

Distributed evaluation without final exam

Assessment Components

designation	Weight (%)
Apresentação/discussão de um trabalho científico	30,00
Teste	70,00
Total:	100,00

Amount of time allocated to each course unit

designation	Time (hours)
Apresentação/discussão de um trabalho científico	30,00
Estudo autónomo	40,00
Frequência das aulas	30,00
Total:	100,00

Eligibility for exams

Students must attend to at least 75% of the theoretical-practical classes, for the preparation, presentation and defense of an oral communication on a topic related to the syllabus taught in lectures.

Calculation formula of final grade

The final evaluation will include the preparation, presentation and defense of an oral communication on a topic related to the syllabus taught in lectures, as well as a final exam. Students must obtain a minimum score on the final written test of 8.6 out of 20.

The presentation and defense of the oral communication will have a weighting factor of 30% and classification of the final exam will have a weighting factor of 70% to the overall score of the course.Studentswithfinal gradeof 9.5 will be approved.

Special assessment (TE, DA, ...)

The final evaluation will include the presentation and defense of an oral communication on a topic related to the syllabus taught in lectures, as well as a final test. The presentation and defense of the oral communication will have a weighting factor of 30% and classification of the final exam will have a weighting factor of 70% to the overall score of the course.

Classification improvement

Improving classification is performed by final exam. The classification of the oral communication will be maintained.

Observations

Speakers of other Latin languages ​​(Spanish, Italian, French…) who are fluent in Portuguese are accepted and these are provided with the exam in English if they wish; additional clarifications may be given. Students fluent in English are accepted, however classes will take place for the whole class in Portuguese and additional support will be provided, namely support material for classes in English.

If there is a need for confinement due to Pandemic COVID19, the following changes can be made:
There should be no changes to the theoretical program or the theoretical-practical program.

Teaching Methods and Learning Activities:

In scenario C, the theoretical classes will be taught at a distance in a synchronous manner. In scenario B, the classes will be simultaneously in person and remotely.
In scenario B and C, exercises related to the theoretical classes will be made available and explained in a synchronous class by Zoom Colibri
In Scenario B, the theoretical-practical classes will be divided into shifts.

Evaluation process and calculation formula for the final classification: The calculation formula will be maintained.