PHAR206 - PHARMACEUTICAL CHEMISTRY-I

Course Description

Introduction to medicinal chemistry, physico-chemical properties of drugs related compounds, receptor and drug receptor interaction, structural features and pharmacologic activity, thereotical aspect of drug design, bioisosterioism, drug metabolism, theoretical applications in drug development and drug discovery, introduction to CNS drugs, adrenergic agents, adrenergic blocking agents, cholinergic agents, cholinergic blocking agents, general and local anesthetics, sedative and hypnotic drugs, tranqulizing agents and neuroleptic drugs, antidepressant and antiepileptic drugs, antiparkinsonian drugs, analgesic and antiinflammatory drugs are covered. Synthesis of some drugs and pharmaceutical raw materials, laboratory safety, yield calculation, thin layer chromatography(TLC), laboratory techniques like filtration, crystallization, extraction, distillation e.g., reaction types like esterification, diazotization. Pharmaceutical Chemistry I Lab. The practical worknow are performed on synthesis of some drugs and pharmaceutical raw materials, laboratory safety, laboratory techniques like filtration, crystallization, extraction, distillation e.g., reaction types like esterification, acylation, nitration, bromination and diazotization.

PHARMACEUTICAL CHEMISTRY-I

Evaluation Tools (Active Term)

No evaluation items have been defined.

Course outcomes

01 Describe structure activity releationship between the receptor/target and the drug
02 Be able to express and analyze molecular structures of the drugs
03 Identify the importance of the stereochemistry of drugs
04 Be able to illustrate IUPAC nomenclature of the medicines
05 Be able to identify working mechanisms and to structure the metabolism of the medicines

Course Syllabus

Week	Topic
Week 1	Explain the fundamental terminology and concepts of drug discovery, including hits, lead compounds, drug candidates, and approved drugs, and describe the major stages of the drug discovery and development process.
Week 2	Explain the principles of molecular recognition in drug–target interactions and identify the major intermolecular forces involved in ligand–receptor binding, including hydrogen bonding, ionic interactions, hydrophobic interactions, van der Waals forces, and π-interactions.
Week 3	Analyze the structural and conformational requirements for optimal ligand–receptor interactions and explain how molecular shape, stereochemistry, flexibility, and conformational complementarity influence biological activity.
Week 4	Explain the thermodynamic principles of ligand binding, including the contributions of enthalpy and entropy to binding affinity, and relate these principles to strategies for optimizing ligand–target interactions.
Week 5	Evaluate the effects of chemical modifications on ligand binding affinity and molecular recognition, including changes in molecular flexibility, hydrophilicity, steric effects, electronic properties, and functional groups.
Week 6	Explain the fundamental principles of pharmacokinetics and describe how absorption, distribution, metabolism, and excretion determine the concentration–time profile and duration of drug action.
Week 7	Explain gastrointestinal tract physiology and the mechanisms of drug absorption, and relate drug ionization, lipophilicity, solubility, molecular size, and formulation to gastrointestinal drug absorption.
Week 8	MIDTERM
Week 9	Explain the principles of drug metabolism and excretion, including Phase I and Phase II metabolic reactions, major drug-metabolizing enzymes, renal excretion, and the factors affecting drug clearance and half-life.
Week 10	Integrate ADME principles to evaluate the pharmacokinetic properties of drug molecules and explain how physicochemical and structural characteristics influence bioavailability, clearance, half-life, and overall drug exposure.
Week 11	Explain the organization and function of the cholinergic system and classify cholinergic agonists and antagonists according to their chemical structures, mechanisms of action, and therapeutic applications.
Week 12	Analyze the structure–activity relationships of selected cholinergic drugs and correlate their chemical structures and physicochemical properties with receptor interactions, pharmacological activity, selectivity, and therapeutic effects.
Week 13	Explain the organization and function of the adrenergic system and classify adrenergic agonists and antagonists according to their chemical structures, receptor selectivity, mechanisms of action, and therapeutic applications.
Week 14	Analyze the structure–activity relationships of selected adrenergic drugs and correlate structural features with receptor interactions, pharmacological activity, selectivity, physicochemical properties, and therapeutic effects.
Week 15	Final Exams

Reference Books & Course Materials

01 Introduction to Medicinal Chemistry
02 Foye's Principles of Medicinal Chemistry

Learning Outcomes

L01 Describe the structure-activity relationship between the receptor/target and the drug SOLO 3
L02 Be able to express and analyze molecular structures of the drugs SOLO 3.5
L03 Identify the importance of the stereochemistry of drugs SOLO 2
L04 Be able to illustrate IUPAC nomenclature of the medicines SOLO 3
L05 Be able to identify working mechanisms and to structure the metabolism of the medicines SOLO 3

Program Outcomes

P01 Gain the ability to apply the Pharmacy profession.
P02 Interpret the accuracy and reliability of the current theoretical and practical knowledge in the field of pharmacy, as well as being able to follow and evaluate innovations.
P03 Practically apply the knowledge they gain on pharmaceutical sciences. The acquired knowledge and skills allow the graduates to act as the closest health consultant to the public with the ability to inform the public.
P04 Evaluate and apply current technology related to basic subjects and principles covering pharmacy and health sciences and take part in in-service training seminars.
P05 Know the risks and evaluation of the use of drugs and other chemicals and safe laboratory practices (GMP).
P06 Acquire the ability to interpret the findings obtained by qualitative and quantitative measurements and to reach valid scientific results from the data.
P07 Prepare pharmaceuticals and provide guidance on the use of pharmaceutical products.
P08 Design research and develop projects related to pharmaceutical products; manage and share the results.
P09 Be competent to accurately and intelligibly communicate and transfer knowledge about prescription content and pharmaceutical products to the patient / user. The graduates are trained on taking necessary precautions for safe drug usage and encouraging rational drug use, as well as providing consultancy and supervision.
P10 Work in an interdisciplinary environment. Graduates can cooperate with other professional groups, participate in vocational training and activities, have proper knowledge and communication skills.
P11 Take part in social responsibility projects related to health. Graduates have awareness on sustainable environment and participate in activities and practices related to their profession.
P12 Open a community pharmacy, also work in hospital pharmacies, can work in different fields related with pharmaceuticals, cosmetics, medical and herbal products, as well as production and quality control in the pharmaceutical industry. Takes part in the professional development of herself/himself, her/his colleagues and pharmacy students.
P13 Implements the legal and professional law and ethics as a health professional, in issues concerning public health.
P14 Knows and applies the processes related to drug design from natural or synthetic sources, as well as development, preparation, analysis and metabolism of drugs in the human body.

Po-Lo Matrix

LO	P01	P02	P03	P04	P05	P06	P07	P08	P09	P10	P11	P12	P13	P14	Average
L01	4	4	4	4	3	3	3	4	3	4	3	3	3	5	3.57
L02	4	4	4	4	4	4	3	3	3	4	3	3	3	5	3.64
L03	4	4	4	4	3	4	3	3	3	4	3	3	3	5	3.57
L04	4	4	4	4	4	3	3	3	3	4	3	3	3	5	3.57
L05	4	4	4	4	4	3	3	3	3	4	4	3	3	5	3.64