ORGANIC PHARMACEUTICAL CHEMISTRY

Course Information
TitleΟΡΓΑΝΙΚΗ ΦΑΡΜΑΚΕΥΤΙΚΗ ΧΗΜΕΙΑ (Ε) / ORGANIC PHARMACEUTICAL CHEMISTRY
CodeΝΠ46
FacultyHealth Sciences
SchoolPharmacy
Cycle / Level1st / Undergraduate
Teaching PeriodSpring
CommonNo
StatusActive
Course ID180000287

Programme of Study: Programme of Studies 2008-

Registered students: 10
OrientationAttendance TypeSemesterYearECTS
CoreElective Courses844

Class Information
Academic Year2018 – 2019
Class PeriodSpring
Faculty Instructors
Weekly Hours4
Class ID
600137852
Type of the Course
  • Scientific Area
Course Category
Specific Foundation / Core
Mode of Delivery
  • Face to face
Language of Instruction
  • Greek (Instruction, Examination)
Prerequisites
General Prerequisites
Physicochemical properties of organic compounds. Basic principles of medicinal chemistry.
Learning Outcomes
Aims of the course: The course is an expansion and in depth analysis of the required course (code number: ΝΠ-38) of the same semester and its aim is the application of modern aspects of medicinal chemistry in drug design and in the successful confrontation of pathologic conditions using contemporary approaches of medicinal chemistry & chemical biology. Specifically: - Scaffolds and physicochemical properties of drug-like molecules. Principles of identification, optimization and production of new chemical entities. - Oxidative stress, antioxidant pharmacotherapy. Oxidative stress and biologic stress in pathologic conditions. Pharmacochemical aspects of biological stress, relations between biological and oxidative stress. Indices of oxidative and biologic stress and their interrelationships. Consequences of oxidative and of biologic stress on health. Skills: By the end of this course, the students will have a working knowledge of: - The three dimensional graphical depiction of compounds using a molecular modeling software. - The structural energy minimization implementing molecular & quantum mechanism. - The two dimensional drawing of compounds and the calculation of distribution & partition coefficients. - The involvement of oxidative stress in pathologic conditions and diseases and the response of the organism to xenobiotics - The physiologic defensive mechanisms as stress response
General Competences
  • Apply knowledge in practice
  • Retrieve, analyse and synthesise data and information, with the use of necessary technologies
  • Adapt to new situations
  • Make decisions
  • Work autonomously
  • Work in teams
  • Work in an international context
  • Work in an interdisciplinary team
  • Generate new research ideas
  • Design and manage projects
  • Appreciate diversity and multiculturality
  • Respect natural environment
  • Demonstrate social, professional and ethical commitment and sensitivity to gender issues
  • Be critical and self-critical
  • Advance free, creative and causative thinking
Course Content (Syllabus)
1) Vassilis Demopoulos Chemical biology in medicinal chemistry, with focus on: a) stereo-chemical factors and biological activity (optical isomerism, spatial isomerism, conformational space) b) physical & chemical properties important in biological activity (lipophilicity, hydrophobicity, ionization, solubility, molecular polar surface area) c) bioisosterism d) thermodynamic analysis of ligand-receptor interactions e) permeability through biological membranes 2) Eleni Rekka In this course, pharmacochemical aspects of oxidative and biologic stress, their indices and their relationships are analysed. Importance of oxidative and of biologic stress in diseases of the modern society, e.g. Alzheimer’s and Parkinson’s diseases, development of biologic stress and other pathologic conditions is examined. Xenobiotic toxicity connected to free radical formation, toxic metabolites, antioxidant intervention are presented. 3) Ioannis Nicolaou Pharmacochemical approach for the management of the lack of selectivity toward tumor cells and low therapeutic index of the antineoplastic agents, via two primary strategies: a) through the design of targeted anticancer prodrugs for tumor site-specific activation, and b) through a tumor-targeting drug delivery system which consists of a tumor recognition moiety (as monoclonal antibodies, polyunsaturated fatty acids, folic acid, hyaluronic acid, and oligopeptides) and a cytotoxic warhead connected directly or through a suitable linker to form a conjugate.
Use of Information and Communication Technologies
Use of ICT
  • Use of ICT in Course Teaching
  • Use of ICT in Communication with Students
Description
1) Vassilis Demopoulos Lectures: The haptics (http://www.telegraph.co.uk/education/educationnews/8271656/Write-it-dont-type-it-if-you-want-knowledge-to-stick.html) approach is used Teaching notes: electronic distribution via USB flash memory. 2) Eleni Rekka Lectures: The haptics (http://www.telegraph.co.uk/education/educationnews/8271656/Write-it-dont-type-it-if-you-want-knowledge-to-stick.html) approach is used 3) Ioannis Nicolaou Lectures, notes, statements etc are presented in the corresponding place of the website of the School of Pharmacy.
Course Organization
ActivitiesWorkloadECTSIndividualTeamworkErasmus
Lectures60
Laboratory Work40
Interactive Teaching in Information Center20
Total120
Student Assessment
Description
- The evaluation of knowledge and skills which have been acquitted by the students from the course work is attested with written examinations (80% of the final grade + 20% of experimental aptitude) which are conducted in a fixed date. The written examinations have duration of 3.5h, and consist of approximately ten (10) composite questions spherically covering the tough subjects. Grading is proportionally allocated to the tutors. - Τhe evaluation process is based on questions that the students are asked to answer based on their knowledge obtained from the lectures as well as on the critical thinking and ability to combine, evaluate and handle the acquired knowledge and information. - During the laboratory work, students hand over a report of their results and are evaluated. Successful termination of the laboratory course permits their participation to the final examination.
Student Assessment methods
  • Written Exam with Short Answer Questions (Summative)
  • Written Assignment (Formative)
Bibliography
Course Bibliography (Eudoxus)
Ε.Α. Ρέκκα, Π.Ν. Κουρουνάκης, «Οργανική Φαρμακευτική Χημεία: Θέματα Φαρμακοχημείας-Σχεδιασμού Φαρμάκων», Εκδ. Φ. Χατζηπάντου, 2010 (ISBN 978-960-98594-3-1)
Additional bibliography for study
1) Βασίλης Δημόπουλος - Richard B. Silverman “The Organic Chemistry of Drug Design and Drug Action”, Academic Press, 2004, ISBN-10: 0126437327 -Joseph J. Cannon “Pharmacology for Chemists”, Oxford University Press, 2007, ISBN-10: 0841239274 - Jonathan M. Goodman “Chemical Applications of Molecular Modelling”, The Royal Society of Chemistry, 1998, ISBN: 0854045791 - M. P. Edwards and D. A. Price, "Role of Physicochemical Properties and Ligand Lipophilicity Efficiency in Addressing Drug Safety Risks". Ann. Rep. Med. Chem., 45: 381–391 (2010) - A. Avdeef, “Physicochemical profiling (solubility, permeability and charge state)”, Curr. Top. Med. Chem., 1, 277-351 (2001) - N. A. Meanwell “Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design”, J. Med. Chem., 54, 2529–2591 (2011) - J. Clayden, S. R. LaPlante et. al. “The Challenge of Atropisomerism in Drug Discovery” Angew. Chem. Int. Ed., 48, 6398 – 6401 (2009) 2) Ελένη Ρέκκα - Ε.Α. Ρέκκα, Π.Ν. Κουρουνάκης, «Οργανική Φαρμακευτική Χημεία: Θέματα Φαρμακοχημείας-Σχεδιασμού Φαρμάκων», Εκδ. Φ. Χατζηπάντου, 2010 (ISBN 978-960-98594-3-1) - R. Rodrigo, “Oxidative Stress and Antioxidants: Their Role in Human Disease”, 2009, Nova Science Pub Inc. 3) Ιωάννης Νικολάου - Journal of Medicinal Chemistry (ACS Publications) - Bioorganic & Medicinal Chemistry Letters - Elsevier - Bioorganic & Medicinal Chemistry (ISSN 0968-0896)
Last Update
22-11-2016