Topic outline

• Welcome to Advanced Medicinal Chemistry & Drug Discovery
  

  Welcome to Advanced Medicinal Chemistry & Drug Discovery

  
  

  
  

  Medicinal chemistry is a discipline that encloses the design, development, and synthesis of pharmaceutical drugs. 

  
  The discipline combines expertise from chemistry, especially synthetic organic chemistry, pharmacology, and other biological sciences.

  
   It is also part of medicinal chemistry the evaluation of the properties of existing drugs.

  
  

   Medicinal chemistry Molecular mechanism  of drug action.
• Course Information
  

  Course Information

  Name of the course: Advanced Medicinal Chemistry & Drug Discovery
  

  Course course: MPH 511

  Total credit : 3

  Program: M. Pharm
  
  
• Course Instructor
  

  Course Instructor

  Professor Abdullah Faruque

  
  
• Rationale
  

  Rationale

  This course will introduce students with the intersection of chemistry, especially synthetic organic chemistry, pharmacology and various other biological specialties, where they are involved with design, chemical synthesis and development  of  bio-active molecules.

  
  

  Learning outcome:
  Relate the structure and physical properties of drugs to their pharmacological activity.
  Demonstrate an understanding of concepts such as drug metabolism, bioavailability and pharmacokinetics.
  Understand the  role of medicinal chemistry in improving these parameters.
  Mechanism of chemical carcinogenesis, role of free radicals in aging and diseases.

  
  

  Course contents: 

  
  

  1. Drug discovery and development
  

  2. Drug design
  3. Molecular mechanism of drug action
  4. Cancer biology and chemical carcinogenesis
  5. Free radicals and anti-oxidants
  6. Macromolecules
  7. Biosynthesis

  • Announcement Forum

    Mark as done
  • Lesson plan Assignment

    Mark as done
  • Course curriculam Assignment

    Mark as done
  • Course outline. Assignment

    Mark as done

    Total marks: 100                                                                                                                 Total credits: 3
    Breakdown of marks
    Assessment types	Number of assessments	Marks in each assessment	Total marks
    Class test	3 class tests	10 marks	10 marks (Average)
    Presentation	1 presentation	5 marks	5 marks
    Attendance	Base on class attendance		5 marks
    Midterm exam	30 marks (Question types: MCQ,T/F, Filling the gaps)		30 marks
    Final exam	30 marks (Question types: MCQ,T/F, Filling the gaps)		30 marks
    Viva	Viva		20 marks
    Total marks:			100

  • Assessment strategy Assignment

    Mark as done
  • Teaching strategy Assignment

    Mark as done
  • Recommended books Assignment

    Mark as done

    Recommended Books:

    1.      An Introduction to Medicinal Chemistry – Graham L. Patrick

    2.      Advanced Practical Organic Chemistry – J. Leonard, B. Lygo & G. Procter

    3.      Advanced Organic Chemistry: Reactions and Mechanisms – Bernard Miller

    4.      March’s Advanced Organic Chemistry – Michael B. Smith & Jerry March

    5.      Mechanism and theory in organic chemistry - Thomas H. Lowry & Kathleen Schueller Richardson

    6.      Foye W, “Principles of Medicinal Chemistry” Lea & Febiger.

    7.      Delgado J.N., Remers WA eds, “Wilson & Giswolds Text Book of organic Medicinal & Pharmaceutical chemistry” Lippincott, New York.

    8.      Alex Gringauz-“Introduction to Medicinal Chemistry” Wiley-VCH, Inc. New York.

    9.       Abraham DJ,ed., Burger’s Medicinal Chemistry & Drug Discovery, Vol-I-VI, John Wiley & sons, New Jersey.

    
    

  • GOOGLE MEET LINK

    Mark as done
• General instructions to students
  

  General instructions to students

  
  

  
  

  • All the students registered for this course have to enroll in Moodle.
  • Students can find all the course materials from Moodle.

  • All the students have to submit the soft copy of their "Assignment" in Moodle under assignment section created here and for this they will be graded here.

  • One discussion or feedback forum is created under each of the lecture Students have to give their feedback on these forum and marks will be given for their feedback

  • Any announcement regarding the class will be posted on Moodle. So they have to keep themselves always active on Moodle.

  • All the quizzes and presentation will be held on online (Moodle) and may be few of the class will be held on face to face class and it will be announced before the class.

  • The question pattern and the syllabus for the quizzes, midterm and final exam is given here under each of the section (quizzes, midterm and final).

  • There are Midterm and Final Examination presentation forum under these sections where students can discuss with each other about their midterm and final exam syllabus, any problem regarding the exam etc.

  
  
• Chapter1 : Drug discovery and development
  

  Chapter1 : Drug discovery and development

  Learning Outcome: 

  Introduce with historical perspective of  Drug discovery and development.
  Learn about generation  and  optimization of lead compound
  Get idea about drug discovery by combinatorial chemistry.
  Use of genomics as a source of drug development.
  
  Topic contents:
  Historical perspective, generation of leads and lead optimization
  Objective of lead optimization, analog approach, cell biology and genomics as a source of drugs.
  Drug discovery by combinatorial chemistry and molecular diversity, development in the drug design.

  • Lecture slide File

    Mark as done
• QUIZ 1
  

  QUIZ 1

  
  
• Chapter 2: Drug design
  

  Chapter 2: Drug design

  Learning Outcome: 

  Learn the  considerations for drug design, estimating individual group  in ligand receptor interactions.
  Come into know about significance of stereochemistry in drug design.
  Get idea about drug discovery by combinatorial chemistry.
  Know the pharmacophoric approach, Pharmacophore based ligand design

  
  
  Topic contents:

  Molecular recognition in drug design

  Stereochemistry and drug design

  Bioisosterism in drug design. 

  Quantitative structure-activity relationships (QSAR) in drug design

  Nucleic acid based drug design
  

  • Lecture slide File

    Mark as done
• MID TERM EXAMINATION
  

  MID TERM EXAMINATION

  
  

  • MID TERM EXAMINATIONMPH 511 Quiz

    Mark as done
• Chapter 3: Molecular mechanism of drug action
  

  Chapter 3: Molecular mechanism of drug action

  Learning Outcome: 

  Learn Structure and classification of receptors.
  Come into know about binding forces in drug enzyme interaction
  Get idea about enzyme stimulation and enzyme inhibition.
  Know the signal transduction mechanisms consequence of drug receptors interaction.

  
  
  Topic contents:

  Drug action and receptors

  Drug action and enzyme

  Drug action and carrier proteins

  Drug action on DNA and RNA.

  
  

  • Lecture slide File

    Mark as done
• Presentation
  

  Presentation

  
  
• Chapter 4: Cancer biology and chemical carcinogenesis
  

  Chapter 4: Cancer biology and chemical carcinogenesis

  Learning Outcome: 

  Introduce with cell cycle.
  Learn mechanism of chemical carcinogenesis.
  Get idea about drug toxicity.

  Understand the design of the toxicity test.
  
  

  
  Topic contents:

  Cell cycle and control, analysis of cell cycle (flow cytometry).

  DNA repair, drug toxicity, the evaluations of toxicity in lower animals.

  Idiosyncrasy and pharmacogenetics.

  Drug allergy in man, test for prediction of drug allergies.

  Design of the toxicity test.

  
  
• QUIZ 2
  

  QUIZ 2

  
  
• Chapter 5 : Free radicals and anti-oxidants
  

  Chapter 5 : Free radicals and anti-oxidants

  Learning Outcome: 

  Get general idea about free radical and anti oxidants.
  Learn mechanism of superoxide theory and oxygen toxicity.
  Get idea about free radicals as useful species.

  Understand the role of free radical in diseases.
  
  

  Topic contents:

  Hydrogen peroxide in biological system, protection against oxidants in biological systems. 

  Lipid peroxidation- a free radical chain reaction, free radical and toxicology.

  Uses of  free radicals.

  Free radical in ageing, arteriosclerosis, ischemic heart disease and neurodegenerative conditions.

  
  
• Chapter 6: Macromolecules
  

  Chapter 6: Macromolecules

  Learning Outcome: 

  General introduction about macromolecules.
  Learn about biological functions of proteins.
  Introduce about factors affecting protein folding.
  Understand chemistry and extraction of nucleic acid.
  
  Topic contents:
  Structure and functions of macromolecules.

  Chemistry of proteins, extraction, isolation and purification, membrane structure, conformation and protein folding.

  Biological functions of proteins and factors affecting protein folding.

  Chemistry of nucleic acids, structure, extraction, isolation and transcription.

  
  
• QUIZ 3
  

  QUIZ 3

  
  
• Chapter 7: Biosynthesis
  

  Chapter 7: Biosynthesis

  Learning Outcome: 

  General introduction about steroidal hormones, alkaloids, carbohydrates and nucleotides.
  Learn about biological functions of steroidal hormones, alkaloids, carbohydrates and nucleotides
  
  

  Topic contents:
  

   Biosynthetic pathways and actions of steroidal hormones, alkaloids, carbohydrates and nucleotides.

  
  
• FINAL EXAMINATION
  

  FINAL EXAMINATION

  
  

  • FINAL EXAM MPH 511 Quiz

    Mark as done
• COMPLEMENTS
  

  COMPLEMENTS