Description of Individual Course Units
Course Unit CodeCourse Unit TitleType of Course UnitYear of StudySemesterNumber of ECTS Credits
300004582008PHARMACEUTICAL CHEMISTRY-IVCompulsory486
Level of Course Unit
First Cycle and Second Cycle
Objectives of the Course
The purpose of the course is to introduce the chemical structures, chemical and physicochemical properties of the drug groups in this course content; to interrelate this properties with pharmaceutic, pharmacokinetic and pharmacodynamic process and structure-activity relations; to teach the synthetic routes used in industry and approaches in synthetic methodology. The aim of the practical course is to introduce the identification of the drug active compounds by spectroscopic methods and to gain application skills.
Name of Lecturer(s)
Assist. Prof. Dr. Zeynep SOYER
Learning Outcomes
11. Being able to understand and interpret the chemical properties causing the pharmaceutical actvity and their relations with biological process.
22. Being able to understand the relations between the chemical structures of pharmaceutically active synthetic and semi-synthetic compounds with therapotic and adverse effects and to predict possible biological responses.
33. Capable of giving examples about drug design methodology and approaches.
44. Being able to understand the chemical structures, chemical and physicochemical properties of the synthetic and semi-synthetic (drug) active compounds.
55. Being able to name the synthetic and semisynthetic molecules’ structure according to the nomenclature rules.
66. Being able to understand the relations between pharmacokinetic properties with chemical structures of the synthetic and semisynthetic molecules used as drug active compound and use this knowledge during the treatment.
77. Being able to understand the relations between pharmacodynamic properties with chemical structures of the synthetic and semisynthetic molecules used as drug active compound and use this knowledge during the treatment.
88. Being able to evaluate the potentials of biological response of the molecules in terms of chemical structure and reactivity.
99. To be able to understand the general chemical structure leading to a pharmacological response and predict the structure activity relationship.
1010. Being able to understand and predict the drug-drug interactions by interrelating pharmacodynamic and pharmakokinetic concept with drugs’ chemical and physicochemical properties in biological systems.
1111. Being able to predict the chemical structures and the possible incompatibilities of activemolecules and excipients and use this knowledge in formulatin and treatment process.
1212. Capable of understanding the basic approaches regarding to the methods of obtaining pharmaceutical active molecules and excipiants and solving possible problems suring synthesis.
1313. Being able to understand and interpret the principles of working with spectral analysis methods.
1414. Being able to recognize the pharmaceutical active compounds by spectroscopic analysis methods and to apply these methods
Mode of Delivery
Face to Face
Prerequisites and co-requisities
None
Recommended Optional Programme Components
Being successful in organic chemistry course is recommended.
Course Contents
Chemotherapotics (Anticeptic and disinfectants, Uriner Anticeptics, Tuberculostatics, Leprostatics, Antibacterial Sülfonamides), Antibiotics, Antifungal drugs, Antiviral drugs, Antiprotozoal drugs, Anthelmintics, Anticancer drugs (alkylating agent, antimetabolites, Anticancer hormones and antibiotics), Hormones (Steroidal and nonsteroidal sex hormones, Thyroid hormones), Vitamins. Demonstration courses in spectroscopic methods are given before practical studies. Then methods of spectroscopic analysis are practically applied on the given samples.
Weekly Detailed Course Contents
WeekTheoreticalPracticeLaboratory
1Chemotherapotics 1. Introduction 2. Classification 2.I. Synthetic Antibacterials 2.1.1. Topically used Synthetic Antibacterials 2.1.1.1. Anticeptic and Disinfectants 2.1.1.1.1. Introduction 2.1.1.1.2. General concepts 2.1.1.1.3. Classification of Anticeptic and disinfectants 2.1.1.1.3.1. Halogens and Halophors 2.1.1.1.3.2. Alcohols 2.1.1.1.3.3. phenols 2.1.1.1.3.4.Epoxide and Aldehydes 2.1.1.1.3.5. Acids 2.1.1.1.3.6. Oxidant Agents 2.1.1.1.3.7 Heavy metals 2.1.1.1.3.8.Dye compounds 2.1.1.1.3.9.Diarylureas, Amidines and biguanides 2.1.1.1.3.10. Surface active compounds 2.1.1.1.3.11. Aminoacridines 2.1.1.1.3.12. Nitrofuran derivatives2.1.1.2. Conservatives 2.1.1.2.2.1.Parahydroxybenzoic Acid derivatives 2.1.1.2.2.2. Other compounds used as conservatives Chemotherapotics 2.1.2. Systemic Synthetic antibacterials 2.1.2.1. Urinary Antiinfectives 2.1.2.1.1. Classification due to chemical structures 2.1.2.1.1.1. 4-Quinolons 2.1.2.1.1.2. Nitrofuran derivatives 2.1.2.1.1.3. Methenamine 2.1.2.1.1.4. Trimethoprim 2.1.2.2. Antimicobacterial drugs Practical spectroscopic analysis
22.1.2.2.1. Antituberculosis drugs 2.1.2.2.1.1. Primary drugs used for tuberculosis treatment 2.1.2.2.1.1.1. synthetic drugs 2.1.2.2.1.1.2. antibiotics 2.1.2.2.1.2. Secondary drugs used for tuberculosis treatment 2.1.2.2.1.3. Other drugs used for tuberculosis treatment 2.1.2.2. Antimicobacterial drugs 2.1.2.2.2.1. Drugs used for Lepra Treatment 2.1.2.2.2.2. Sulphones and structure-activity relationships 2.1.2.2.2.3. Clofazimine 2.1.2.2.2.4. thalidomide 2.1.2.3. Antibacterial sulfonamides 2.1.2.3.3.1. Current status of therapeutic effects of antibacterial sulfonamides 2.1.2.3.2. Contributions of Sulfa drugs to drug chemistry 2.1.2.3.3 Classification of Antibacterial sulfonamides 2.1.2.3.3.1. Systemic Antibacterial sulfonamides 2.1.2.3.3.4. Topically used Antibacterial sulfonamides 2.1.2.3.4. General synthesis method of Antibacterial sulfonamides 2.1.2.3.5. Structure activity relatonship of Antibacterial sulfonamides 2.1.2.3.6. Mechanism of action of Antibacterial sulfonamides 2.1.2.3.7. Metabolism of 2.1.2.3.8. Antibacterial sulfonamides Prodrugs facilitate drug intake Practical spectroscopic analysis
3Antibiotics 1. Introduction 2. Classification of antibiotics I. β –Lactams 1. Penisillins a) Structure oriented complications of penicillins b) Brief history of penicillin c) Transition to semi-synthetic penicillins d) Methods of obtaining semi-synthetic penicillins e) β-Lactamase Resistant Penicillins f) Acid Resistant Penicillins g) Antipseudomonal Penicillins h) Geniş Spektrumlu Üreidopenisilinler i) Penicillins’ mechanism of action j) Structure-activity relationship of penicillins k) Metabolism of penicillins Ultraviolet(UV) demonstration
4Antibiotics 1. Cephalosporins a) Complications of cephalosporins due to structure b) Classification of cephalosporins  First generation cephalosporins  Second generation cephalosporins  Third generation cephalosporins  Forth generation cephalosporins c) Structure-activity relationship of cephalosporins 2. Monocyclic β-Lactams  Nocardicins  Monobactams • Structure-activity relationship of Monobactams 3. Penems and Carbapenems  Penems  Carbapenemler • Mechanism of action of Carbapenems 5. β-Lactamase Inhibitors Infrared(IR) demonstration
5Antibiotics I. Tetracycline 1. Introduction 2. Chemical structure and nomenclature of Tetracyclines 3. Structure-activity relationship of Tetracyclines 4. Mechanism of action of Tetracyclines II. Amphenicols 1. Chloramphenicol a) Structure-activity relationships b) Synthesis of Chloramphenicol c) Prodrugs of Chloramphenicol Antifungal Drugs A. Introduction B. Classification of Antifungal Drugs I. Topically used drugs in dermatophytosis 1. Synthetic drugs a) Structurally non-specific drugs (Undecylenic acid, tolnaftate, Ciclopirox) b) Alylamines (naftifine, terbinafine) c) Benzylamines (butenafine) d) Azoles (clotrimazole, miconazole, econazole, izoconazole, sulconazole, thioconazole, oxyconazole, ketoconazole, terconazole) 2. Natural drugs (nistatine, pimaricine) 1H NMR demonstration
6Antifungal drugs I. Systemic Drugs used for Micosis treatment 1. Synthetic drugs a) Alylamines (terbinafine) b) Azoles  İmidazoles (ketoconazole)  Triazoles(fluconazole,voriconazole,itraconazole)  Nukleoside analogs (flucitocine) 2. Natural drugs (griseofulvin, amphfotericin B, nistatin) Antiviral Drugs A. Introduction B. Classification of Antiviral Drugs I. Drugs used for prophylaxis 1. Drugs preventing viruses entering the host 2. İmmunostimulants and vaccines 1H NMR demonstration
7Antiviral Drugs I. Antiviral drugs used fort he treatment 1. Antimetabolites a) Derivatives obtained by preserving the sugar of natural purines and pirimidines while making some structural changes in basic part (idoxuridine, triflouridine) b) Derivatives synthesized by attaching natural purine and pirimidine nukleosides to pentoses which are not found in natural nucleosides (vidarabin, cytarabine) c) Compounds obtained by attaching non-sugar substituents which to natural nucleosides.  Purine nucleoside compounds and analogs (acyclovir, 6-deoxyacyclovir, valacyclovir, pencyclovir, famcyclovir)  Pirimidine nucleoside compounds and analogs (zidovudin, sidofovir)  Derivatives bearing heterocyclic rings other than purin and pirimidine (ribavirin) 13C demonstration
8Antiprotozoal Drugs A. introduction B. classification I. Amebicides and tricomoniasis 1. Chemotherapeutics used for Amibiasis a) Drugs used at Asymptomatic phase  5-Nitroimidazoller  8-Hydroxyquinolines  Haloacetamides b) Drugs used at symptomatic phase  Drugs used for intestinal Amibiasis • 5-Nitroimidazoles • 8- Hydroxyquinolines • Ipecac Alcoloids  Drugs used for Extraintestinal Amibiasis • 5-Nitroimidazoles • ipecac Alcoloids • Some antibiotics(paromomicine) • Some 4-aminoquinolines Mass spectroscopy
9Antiprotozoal Drugs I. Leishmaniasis 1. Pentavalan Antimon compounds 2. Aromatic Amidines 3. natural antibiotics like Amphotericine B and Paromomicine 4. Promising new drugs II. trypanosomiasis 1. Nifurtimox 2. Amidines: Pentamidine 3. Suramin 4. Organic arsenic drugs: Tryparsamide, Melarsoprol 5. 2-Nitroimidazoles: Benznidazole 6. some 5-Nitrofuran derivatives 7. someı 8-Aminoquinolines 8. Some antibiotics Multicomponent demonstration
10Midterm exam
11Antiprotozoal Drugs I. Drugs used for Toxoplasmosis II. Antimalarial drugs 1. introduction 2. Antimalarial chemotherapeutics  4-Aminoquinolins: chloroquine, Hydroxy chloroquine  Quinolinomethanol derivatives: Mefloquine  1,4-Naftoquinon derivatives: Atovaquone  Biguanides: Proguanil  1,2-dihydrotriazines: cycloguanil  2,4-Diaminopirimidines: Primethamine  Sulphones: Dapson  Sulphonamides: Sulfadiazine, Sulfadoxin, Sulfisoxazole, Sulfametoxypiridazine  Antibiotics: Doxycyclin  8-aminoquinolines: Primaquine, Pamaquine  9-aminoacridines: quinacrine  phenantren derivatives: Halophantrin 3. developing Antimalarial drugs 4. mechanism of action of Antimalarial drugs Quantitative analysis of multicomponent
12Antihelmintic drugs A. Introduction B. Classification 1. Chematherapeutics used for helminthiasis caused by Nematodes  Benzimidazoles  İmidazothiaazoles  Vinylpirimidines  Piperazine and its analogs  Cyanide dyes  Other Antinematode Molecules 2. Chematherapeutics used for helminthiasis caused by Sestodes  Halogenated Bisphenol derivatives  Halogenated Salisilanilide derivatives  Other Antisestode compounds 3. Chematherapeutics used for helminthiasis caused by Trematodes  Antimon Compounds  Thioxsantenones  Nitro Compounds  Tetrahydroquinolines  Hexahydropirazinoquinolines  Pirazinoisoquinolines Quantitative analysis of multicomponent
13Drugs against Ectoparasites A. Scabies and Pediculocides I. Hydrocarbons with chlor atom II. Pyrethroids III. Comğpounds with sulfur atom IV. Othet drugs Anticancer Drugs A. Introduction B. Classification of Anticancer drugs I. Alkylating agents (Radiomimetics)  Mustards with nitrogen atom  Etylenimines (aziridines)  Methansulphonic aside esthers  Nitrosoureas  Metylhidrazine and triazenoimidazole derivatives  Platinum coordination complexes Practical spectroscopic analysis
14Anticancer drugs I. Antimetabolides  Folic acid antagonists  Purine Antagonists  Pirimidine Antagonists II. Carcinolytic antibiotics III. Mitosis inhibitors IV. Hormones V. Other derivatives Practical spectroscopic analysis
15Vitamins A. Introduction B. Classification I. Fat-soluable vitamins (Vitamin A, D, E, K) Water-soluable vitamins (Vitamin B1 (Thiamine), Vitamin B2 (Riboflavin), Vitamin B3 (Niasin), Vitamin B5 (Pantothenic Acid), Vitamin B6 (Pyridoxal, Pyridoxine), Vitamin B9 (Folic Acid), Vitamin B12 (Cobalamin), Vitamin H (Biotin), Vitamin C (Askorbic Acid) Compensation
16Final
Recommended or Required Reading
1.İlaçların Tanınması ve Kantitatif Tayini, Prof. Dr. Nedime Ergenç, Prof. Dr. Aysel Gürsoy, Prof. Dr. Öznur Ateş, İstanbul Üniversitesi Yayınları, İstanbul, 1966. 2.Türkiyede Üretilen İlaç Etken Maddeleri, Prof. Dr. Nedime Ergenç, Prof. Dr. Serpil Salman, Prof. Dr. Aydın Salman, İstanbul Üniversitesi Yayınları, İstanbul, 1992. 3.İlaçların Metabolizması (Biyotransformasyon), Prof. Dr. Sevim Rollas, Marmara Üniversitesi Yayınları, İstanbul, 1992. 4.Farmasötik Kimya Ders Kitabı Cilt I (Medisinal Kimya), Prof. Dr. Nedime Ergenç, Prof. Dr. Aysel Gürsoy, Prof. Dr. Öznur Ateş, İstanbul Üniversitesi Yayınları, İstanbul, 1997. 5.Farmasötik Kimya Cilt I, Prof.Dr.Hakkı Erdoğan ve arkadaşları, Irmak Matbaası, Ankara, 2000. 6.Farmasötik Kimya Cilt II, Prof.Dr.Hakkı Erdoğan ve arkadaşları,Irmak Matbaası, Ankara, 2000. 7.Farmasötik Kimya Prof.Dr.Hakkı Erdoğan ve arkadaşları, Hacettepe Üniversitesi Yayınları, Ankara, 2004.
Planned Learning Activities and Teaching Methods
Assessment Methods and Criteria
Term (or Year) Learning ActivitiesQuantityWeight
SUM0
End Of Term (or Year) Learning ActivitiesQuantityWeight
SUM0
SUM0
Language of Instruction
Turkish
Work Placement(s)
None
Workload Calculation
ActivitiesNumberTime (hours)Total Work Load (hours)
Midterm Examination111
Final Examination122
Attending Lectures14342
Laboratory14342
Self Study14228
Individual Study for Mid term Examination12525
Individual Study for Final Examination13030
TOTAL WORKLOAD (hours)170
Contribution of Learning Outcomes to Programme Outcomes
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LO1      5      4       
LO2 5          44 3 2   
LO3 3     35          43
LO4 4    5      3 2     
LO5 2    4             4
LO6 3          55       
LO7 3          55       
LO8      55             
LO9      555            
LO10            55 2     
LO11            55 2 2   
LO12        5 4       4  
LO13          5       5 4
LO14          5       5 4
* Contribution Level : 1 Very low 2 Low 3 Medium 4 High 5 Very High
 
Ege University, Bornova - İzmir / TURKEY • Phone: +90 232 311 10 10 • e-mail: intrec@mail.ege.edu.tr