Course

Unit 1

UNIT-I 10Hrs

Study of Natural products as leads for new pharmaceuticals for the following class of drugs

1. Drugs Affecting the Central Nervous System: Morphine Alkaloids (2 hrs)
2. Anticancer Drugs: Paclitaxel and Docetaxel, Etoposide, and Teniposide (2 hrs)
3. Cardiovascular Drugs: Lovastatin, Teprotide, and Dicoumarol (2 hrs)
4. Neuromuscular Blocking Drugs: Curare alkaloids (1 hr)
5. Anti-malarial drugs and Analogues (1 hr)

1. Chemistry of macrolide antibiotics (Erythromycin, Azithromycin, Roxithromycin, and Clarithromycin) and β- Lactam antibiotics (Cephalosporins and Carbapenem) (2 hrs)

Unit 2

UNIT-II 12Hrs

1. Alkaloids:

Preliminary Reading: General introduction, classification, isolation, and purification of alkaloids

Molecular modification and biological activity of alkaloids, general methods of structural determination of alkaloids, structural elucidation and stereochemistry of ephedrine, emetine, and reserpine (6 hrs).

b) Flavonoids:

Preliminary Reading: General introduction, classification

Isolation and purification of flavonoids, General methods of structural determination of flavonoids; Structural elucidation of quercetin (2 hrs).

1. Steroids: General introduction, Stereochemistry, and nomenclature of steroids, Chemistry of sapogenin, cardiac glycosides, contraceptive agents male and female sex hormones (Testosterone, Estradiol, Progesterone), and Vitamin – D (4 hrs).

Unit 3

UNIT-III 12Hrs

1. Terpenoids:

Preliminary Reading: Classification, isolation

Isoprene rule and general methods of structural elucidation of Terpenoids; Structural elucidation of drugs belonging to mono (citral, menthol), di (retinol, Phytol) and tri terpenoids (Squalene) carotenoids (β carotene) (8 hrs).

1. Vitamins: Chemistry and Physiological significance of Vitamin B1, B2, B12, C, E, Folic acid, and Niacin (4 hrs).

Unit 4

UNIT-IV

a) Recombinant DNA technology and drug discovery 11Hrs

DNA technology, hybridoma technology, New pharmaceuticals derived from biotechnology; Oligonucleotide therapy (4hrs).

Gene therapy: Introduction, Clinical application and recent advances in gene therapy, principles of RNA & DNA estimation (4 hrs).

b) Active constituent of certain crude drugs used in the Indigenous system

Diabetic therapy– Gymnema sylvestre, Salacia reticulate, Pterocarpus marsupiam, Swertia chirata, Trigonella foenum graccum;

Liver dysfunction – Phyllanthus niruri; Antitumor – Curcuma longa Linn. (3 hrs)

The subject is designed to provide detailed knowledge about the chemistry of medicinal compounds from natural origin and general methods of structural elucidation of such compounds. It helps to acquire in-depth knowledge of the isolation, characterization, and synthesis of bioactive compounds from natural sources. It also emphasizes gaining expertise in utilizing advanced analytical techniques for the identification and quantification of natural products, such as spectroscopy, chromatography, and spectrometry.

It enables to explore the pharmacological significance of natural products and their potential applications in drug discovery and development and also fosters a curiosity-driven mindset to explore the diverse world of natural products, encouraging continuous learning and exploration. It imparts to develop an attitude conducive to interdisciplinary collaboration, recognizing the interplay between chemistry, pharmacology, and other related fields. Develop leadership qualities with a focus on contributing to advancements in the field of natural product chemistry and pharmaceutical research.

Upon successful completion of the subject student shall be able to; KNOWLEDGE

K1: Explain the importance of natural compounds as lead molecules for new drug discovery. K2: Analyze different types of natural compounds and their chemistry and medicinal importance.

K3: Assess the concept of the rDNA technology tool for new drug discovery.

K4. Evaluate the diverse chemical structures of natural products, including alkaloids, terpenoids, flavonoids, and steroids, integrating knowledge of their biological activities.

K5: Demonstrate advanced understanding of the isolation, purification, and characterization techniques specific to natural product chemistry.

K6: Interpret the active constituents of certain crude drugs used in the indigenous system.

SKILL

S1: Apply the basic techniques and different methods of extraction of phytoconstituents. S2: Identify the active constituents isolated from the crude drugs by chemical methods. S3: Determine the degradation products of different phytoconstituents.

S4: Design the isolation, and purification, of simple chemical constituents from natural sources. S5: Display proficiency in isolation and its spectral characterization.

S6: Apply the analytical techniques for the identification of phytoconstituents

ATTITUDE

A1: Improve self-awareness and personal growth.

A2: Cultivate leadership qualities and skills relevant to the pharmaceutical aspects of natural product development and research.

A3: Enhance critical thinking skills tailored to the analysis and synthesis of information pertinent to natural product chemistry

A4: Embrace a lifelong learning mindset.

A5: Exhibit self-motivation and the ability to engage in self-directed learning.

A6: Display a proactive approach to problem-solving, embracing challenges, and proposing effective solutions.

REFERENCE BOOKS:

1. Chatwal Organic Chemistry of Natural Products Vol I and II.5^th ed. Himalaya Publishing House; 2019.
2. Agarwal Organic Chemistry of Natural Products Vol I and II. 5^th ed. Meerut: Krishan Prakashan Media(P)Ltd; 2019.
3. Purohit SS. Biotechnology: Fundamentals and Applications.13^th Agro-Bios; 2012.
4. Peach K, Tracy Modern Methods of Plant Analysis, Vol I-VII.1^st ed.Springer-Verlag Berlin and Heidelberg GmbH & Co. KG; 2011.

5. Harborne Phytochemical Methods: A Guide to Modern Techniques of Plant Analysis. 3^rd ed. London: Springer-Chapman & Hall 1998.
6. Runeckles Recent Advances in Phytochemistry Vol. I to IV. 3^rd ed. Newyork: Springer Science & Business Media;2012.
7. Finar Organic Chemistry Vol I and II. 5^th ed. New York: Pearson Education India;2002.
8. Vyas SP, Dixit Pharmaceutical Biotechnology.2^nd ed. India: CBS Publishers and Distributors Pvt Ltd; 2019

JOURNALS

1. Journal of Natural Products (American Chemical Society –ACS Publishers) https://pubs.acs.org/journal/jnprdf
2. Natural Products and Bioprospecting (Springer) https://link.springer.com/journal/13659
3. Phytotherapy Research (Wiley) https://onlinelibrary.wiley.com/journal/10991573
4. Natural product reports (Royal Society of Chemistry) https://www.org/journals-books-databases/about-journals/npr/
5. Planta Medica (Thieme Publishers) https://www.in/planta-medica

ASSIGNMENTS:

• New drug development following categories from natural product source
  • Antimalarial
  • Beta-lactam antibiotics
  • CNS agents
• Enrichment of the following class of phytochemicals with examples
  • Alkaloids
  • Polyphenolics
• Terpenoids and biological activities