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Medicinal Chemistry 1 *

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    • An-Najah National University
      College of Medicine and Health Sciences
      Department of Pharmacy
      First Semester 2024/2025
       

       

      Course Name: Medicinal Chemistry 1
      Course Num. : 7303301
      Instructor: Dr. Mohyeddin Assali
      Design Semester: First Semester 2024-2025
       
      Course Description:
      The aim of this course is to introduce the basic concepts of medicinal chemistry. Study the physicochemical properties of the drugs and study their distribution, metabolism and excretion. The course will discuss specific drug classes by covering its chemistry, some synthesis, mechanism of action and its structural activity relationship (SAR).
       
      Course Objectives:
      At the end of this course, learner should be able to:
      • Recognize the relation between the drug chemical structure and its biological activity in the body.
      • Recognize the importance of organic functional groups in determining the physicochemical properties of the drug.
      • Understand the interactions drug-protein, drug-enzyme, and drug-receptor.
      • Know how the body interacts and makes changes on the chemical structure of the drug.
      • Introduce various classes of therapeutic agents with the emphasis on their structure activity relationship (SAR).
       
      Textbook:
      Graham L. Patrick (2012) :  An Introduction to Medicinal Chemistry, fifth edition, OUP Oxford.

       

      Facebook Page:
      https://www.facebook.com/pages/Medicinal-chemistry-course-DrMohyeddin-Assali/612111792144306?ref=hl

       

       

      To see the full course outline ... Click Here

  • Med Chem I all slides 2023-2024

  • Med chem I 2nd semester 2025 8-10

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  • Project med chem I 2nd semester 2024-2025

  • Topic one

    Topic One: Introduction to Medicinal Chemistry & Introduction to Drug Targets “Chapters 1 & 2”
    •  
      Introduction:
      This topic is divided to two chapters; in the first one we will cover the essential concepts used in medicinal chemistry, understand the principle steps of drug discovery and design, discuss the classification system of drugs and how to name drugs. In the second chapter we will have an overview of drug targeting and the essential intermolecular bond forces and interactions.

       

      Objectives:
      At the end of this topic, learner will be able to:
      • Define the main concepts in medicinal chemistry and know the history of medicinal chemistry
      • Understand the mean of drug discovery, structure-activity relationship, Quantitative structure activity relationship, pharmacophore, molecular modeling and combinatorial chemistry in drug design.
      • Know and discuss the stages to discover a new drug and the process of patent it with its regulatory affairs.
      • Discuss the different classification ways of drugs & the process of naming drugs.
      • Define the main drug targets structure & discuss the binding forces between the drug and its binding site.
         
      Plan:
      First: Study the following power point presentation
    • resource icon
      File
      Topic 1 (chapters 1 and 2) File
    •  
      Second: Watch the following videos about combinatorial chemistry and pharmacophore.


        

    •  

  • Topic two

    Topic Two: Introduction to Medicinal Chemistry & Introduction to Drug Targets “Chapter 3, 4 & 5”

    • Introduction:

      This topic is divided into three chapters; in chapter three we will cover proteins as drug targets, review the structure of protein, its building blocks and protein function. In the fourth chapter we will cover enzymes as drug targets. We will study the different types of drugs that can inhibit the enzyme functions “reversible, irreversible, allosteric, transition state inhibitors and suicide substrate” with the demonstration of various examples. In the fifth chapter we will cover receptors as drug targets; this chapter explains the function of receptors, substrate binding sites. Design receptor agonists and antagonists.


    • Objectives:

      At the end of this topic, learner will be able to:

      • Review and understand the primary, secondary, tertiary and quaternary structures of protein and their functions.

      • Know the function of enzymes and how they work

      • Understand How to design irreversible inhibitors of enzymes, suicide substrates or allosteric and transition state inhibitors.

      • Know and discuss the receptor functions and the essential requirements for its messenger binding.

      • Understand how we can design agonists and antagonist depending of the functional binding groups of the drug.

      • Analyze and illustrate various examples of drug agonists and antagonists.


      Plan:

      First: Study the following power point presentation.

    • resource icon
      File
      topic 2 File


    •  

      Second: Watch the following videos about:

      1) Protein Structure and Function

       

  • Topic three

    Topic Three: Drug Functional Groups “Chapter 6”

    •  

      Introduction:

      Inside this topic we will cover the main functional groups that are involved in drug structures and play essential roles in their functions and interaction with the binding sites in the biological receptors and we will focus on the bioisosteres groups that are used in medicinal compounds.


      Objectives:

      At the end of this topic, learner will be able to:

      • Review the main functional groups

      • Knowledge of nitrogen containing functional groups, oxygen containing functional groups, aromatic hydrocarbons and phenols.

      • Knowledge of functional derivative of carboxylic acid, carbonates, carbamates, and ureas.

      • Understand the heterocycles and their effect on the medicinal compounds

      • Understand the bioisoesters groups and their importance in designing new drugs.


      Plan:

      First: Study the following power point presentation.

    • resource icon
      File
      Topic 6 File

  • Topic Four

    Topic Four: Pharmacokinetics “Chapter 7”

    •  

      Introduction:

      In this topic we will talk about how the body interacts and makes changes on the chemical structure of the drug, we will study the ionization of drug molecules, drug partition coefficient and their effects on the drug absorption and distribution, then in a second part we will discuss the biological factors affecting drug metabolism and the two essential phases in metabolic reactions and their effects on the excretion.

       

      Objectives:

      At the end of this topic, learner will be able to:

      • Describe the physicochemical properties of drugs and its roll in drugs absorption to blood circulation and crossing of system barriers

      • Identify The Henderson-Hasselbalch Equation in calculating the drug ionization and its effect on drug absorption

      • Describe importance of water solubility of drug and relate it to its chemical structure.

      • Define the biological factors that affect the drug metabolism

      • Define the different phases of drug metabolism in the body (phase I and phase II) with their different chemical modifications.

       

      Plan:

      First: Study the following power point presentation.

    • resource icon
      File
      Topic 7 File

  • Topic Five

    • Topic Five: Anti-Infective Agents “Chapter 8A & B”

       

      Introduction:

      In this topic we will talk about disinfectants & antiseptics agents, also we will all the classes of antibacterial agents and antibiotics. These classes are classified to sections, in each section we will study their different classes, structure-activity relationship and the proposed mechanism of actions. 

       

      Objectives:

      At the end of this topic, learner will be able to:

      • The capability to distinguish the different types of the desinfectants and antiseptics drugs.

      • Define the different classes of antibiotics and their SAR studies.

      • The possibility to identify the essential functional binding groups in antibacterial drugs

      • Describe the different subgroups of antibacterial groups, and the capability to design and modify the structures of these drugs.

         

      Plan:

      First: Study the following power point presentation.

    • resource icon
      File
      topic 8 File

    • Second: Watch the following videos about:

      1) The mechanism of action of B-lactams antibiotics and resistance

       

      2) The mechanism of action of fluoroquinolones

       

  • Topic six

    • Topic Six: Anti-Fungal Agents, Anti-Protozoal Agents, Anthelmentics & Anti-Malarial Agents “Chapter 8C,D,E & F”

       

      Introduction:

      In this topic we will cover Anti-fungal agents, Anti-protozoal Agents, Anthelmentics & Anti-malarial agents. This topic will include the different classes of anti-fungal agents “Fatty acids, Phenols, Nucleoside antifungals, Antifungal antibiotics, other antifungal antibiotics, Allyamines, Azoles”. We also will discuss the different classes of anti-protozoal, anthelmentics and the antimalarial drugs.

       

      Objectives:

      At the end of this topic, learner will be able to:

      • Describe the structure of the fungus.

      • Classify the different classes of antifungal drugs.

      • Understand and distinguish between the different groups of antifungal drugs.

      • Define the structure of the protozoa and the drugs used against them

      • Describe SAR and the drugs used as anthelmentics and antimalarial drugs

       

      Plan:

      First: Study the following power point presentation.

    • resource icon
      File
      Topic 6 (chapter 8 c-f) File

    • Second: Watch the following video about the mechanism of action of amphotericin B

       

  • Topic seven

    • Topic Seven: Anti-Viral Agents “Chapter 8G”

       

      Introduction:

      In this topic we will cover antiviral agents. This topic will include the structure of a virus and its life cycle. We will talk also about the antiviral agents in general and that used against DNA viruses. In another part we will discuss antiviral agents acting against RNA viruses “HIV, flu virus, cold virus”. 

       

      Objectives:

      At the end of this topic, learner will be able to:

      • Distinguish the different types of the desinfectants and antiseptics drugs.

      • Define the different classes of antibiotics and their SAR studies.

      • Identify the essential functional binding groups in antibacterial drugs

      • Describe the different subgroups of antibacterial groups, and the capability to design and modify the structures of these drugs.

      Plan:

      First: Study the following power point presentation.

    • Second: Watch the following video about how HIV infects host cells.


    • resource icon
      File
      topic 7 (chapter 8g) File

  • Topic eight

    • Topic Eight: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) “Chapter 9”

       

      Introduction:

      In this topic we will cover NSAIDs drugs. This topic will include the mechanism of the inflammations and the role of COX-1 and COX-2 in the process. Then we will discuss how to design anti-inflammatory drugs based on the two COX isozymes. After that, we will talk about different classification of these drugs and their structure activity relationship. 

       

      Objectives:

      At the end of this topic, learner will be able to:

      • Describe the process of inflammation

      • Understand the role of COX-1, COX-2 and prostaglandins in the inflammation.

      • Distinguish between the two isozymes (COX-1 & COX-2) and learn how to design specific inhibitors.

      • Classify the different types of NSAIDs drugs and the ability to distinguish their actions

      • Enable to identify each structure activity relation of each group of the NSAIDs. 

         

      Plan:

      First: Study the following power point presentation.

    • resource icon
      File
      Topic 9 File

  • topic 10: steroidal anti-inflammatroy drugs

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