Department of Pharmaceutical & Medicinal Chemistry (D073)

DEPARTMENT OF PHARMACEUTICAL AND MEDICINAL CHEMISTRY (PMC) COURSE DESCRIPTION FOR PHARMD PROGRAMME 

Structural and Inorganic Pharmaceutical Chemistry (2 Units)                                                PMC 231
  • Atomic and Molecular structure: A short review of electronic structure of atoms and molecules including introduction of quantum theory, application of Schrödinger equations to simple systems (e.g. the Hydrogen atom) to show the origin of the: n, l, m, s, nomenclature. The relationship between the electronic structure of elements and the formation of covalent, ionic and coordinate (dative) bonds leading to complexation and chelation. Their nature and pharmaceutical importance.
  • A brief review of fundamental concepts in organic chemistry such as bonding and reactivity of organic compounds, hybridization, resonance theory, inductive, mesomeric, hyper conjugative and electromeric effects.
  • A comparative study of the physico-chemical properties, preparation and uses of the elements of the periodic table and their compounds of pharmaceutical importance, including the transition elements. The chemical basis for the pharmaceutical uses will be emphasized.
Physical Pharmaceutical Chemistry (2 Units)                                                              PMC 232
  • Review of principles of thermodynamics and chemical kinetics relevant to pharmacy.
  • Effect of these on the feasibility of drug synthesis, mixing, solubility, biological redox systems.
  • Review of principles of chemical and ionic equilibria kinetics relevant to pharmacy.
  • Physical properties of drug molecules viz: dipole moment, optical activity, surface tension, viscosity, adsorption, melting point.
Practical Physical and Inorganic Pharmaceutical Chemistry (1 Unit)              PMC 234
  • Experiments to cover the physical properties of drug molecules and chemical kinetics, which include Adsorption from solutions; The use of polarimeter; The use of tensiometer; The use of viscometer; Chemical kinetics; Determination of melting point; Gravimetry
  • Experiments to cover inorganic pharmaceutical qualitative analysis; Cation analysis; Identification of acid radicals.
Organic Pharmaceutical Chemistry (3 Units)                                                              PMC 331
  • General review of organic reactions leading to interconversion and modification of functional groups through nucleophilic and electrophilic substitution, elimination addition and rearrangement reactions. Utility of these reactions for isolation, characterization, elucidation of structure and synthesis of medicinal products.
  • Chemistry of Organometallic compounds: Organo Lithium; Organo Magnesium (Grignard reactions). Their reactions and applications in organic synthesis. Application of co-ordination compounds, metal complexes and chelating agents will be discussed.
  • Types of organic reaction mechanisms taken in relation to types of organic functional groups, effects on their stability, use in pharmacy, other physiochemical properties, solubility, absorption, distribution, and excretion when found in drug molecules.
  • Alcohols and phenols, carboxylic acids, and their derivatives (amides, esters, acid anhydrides, acyl halides) and sulphonic acid, also to be treated are amines and imines, nitriles, nitro and nitroso group and azo-compounds.
  • Chemistry of Heterocyclic compounds. General introduction, structure, nomenclature, and synthesis of five membered ring heterocycles viz: pyrol, furan thiophene, imidazole etc. Examples of drugs in current use containing such heterocycles should be cited.
  • Stereochemistry: Review of total concept of stereoisomerism as distinct from isomerisms of other types-optical and geometrical isomerism chiral and achiral molecules, stereoisomerism and molecular conformation in examples, Determination of configuration – spectroscopic methods Resolution of racemic mixture and importance in Pharmacy using named medicinal examples. Optical rotatory dispersion and its uses. Importance of stereochemistry in terpenes.
Pharmaceutical Specification and Standardization (2 Units)                                       PMC 332
  • Official standards for pharmaceutical chemicals and formulated products which are designed primarily to set limit of tolerance for the product at the time it reaches the patient. Such quality criteria which are specified in official monographs for pharmaceutical chemicals include: A description of the drug or product, Solubility, Test for identity, Physical constants,
  • Quantitative assay of pure chemical entity in the case of pharmaceutical chemicals, or of the principal active constituents in the case of formulated product, The methods mentioned above should include: Acid-base titrations, non-aqueous, iodometry, iodimetry, oxidation-reduction titrations, complexometric titrations, gravimetry
  • Electrochemical methods such as potentiometry, conductometry, coulometry, voltammetry etc.
  • Limit tests
  • The sources of impurities in pharmaceutical products. Limit test to exclude excessive contamination, and Storage condition.
Drug Syntheses (2 Units)                                                                                 PMC 336
  • Basic techniques in syntheses such as reflux, crystallization, purification etc., Sources of starting materials/intermediates. Use of protective groups. Design of synthetic process such as retro synthesis, asymmetric synthesis.
  • Overview of combinatorial chemistry, green chemistry.
  • Reagents and facilities in synthesis.
  • Safety issues in synthesis.
  • Organic Synthesis on medicinal compounds involving several stages, e.g., preparation of benzocaine (Ethyl-p-aminobenzoate); Preparation of Aspirin; Preparation of sulphanilamide, Acetaminophen etc.
  • Synthesis of polypeptides and immunologicals.
  • General introduction, structure, nomenclature, and synthesis of six-member ring heterocycles viz: pyridine, piperidine, quinoline and isoquinoline. Examples of drugs in current use containing such heterocycles should be cited
Practical Pharmaceutical Qualitative Analysis (1 Unit)                                                           PMC 334
  • Experiments to cover organic and inorganic pharmaceutical qualitative analysis, which include: Qualitative organic analysis;
  • Chemical tests; Physical and chemical properties of individual members of functional group classes.
Instrumental Methods in Pharmaceutical Analysis (2 Units)                          PMC 431
  • Instrumental methods for quantitative analysis of pharmaceuticals: UV-Visible spectrophotometry; Flame photometry, Atomic Absorption spectroscopy, Fluorimetry;
  • Electrochemical methods such as Polarography, conductometry, voltammetry, potentiometry and Karl Fisher titrimetry
  • Instrumental Methods for structure elucidation of drugs and natural products: Infra-Red spectroscopy; 1D and 2D NMR Spectroscopy; Mass Spectrometry; Gas-liquid chromatography; HPLC; Hyphenated techniques like GC-MS, LC-MS, and LC-NMR etc.
  • Other methods; polarimetry, refractometry etc.
Practical Pharmaceutical Analysis (1 unit)                                                       PMC 433

Experiments will cover the areas covered in the theory classes

Practical Drug Synthesis (1 unit)                                                                     PMC 435

Experiments will cover the areas covered in the theory classes

Medicinal Chemistry (2 Units)                                                 PMC 432
  • General introduction to medicinal chemistry, introduction to drugs, their actions and discovery, classification of drugs, drug structure and solubility
  • Chemistry of drug metabolism.
  • General principles. Characteristics of photochemical reactions and applications both in the synthesis and spoilage of drugs.
  • Structure Activity Relationships
Drug Design and Development (2 Units) PMC 532
  • Overview of approaches in drug design (Bioprospecting etc.)
  • Drug design: Physico-chemical approaches to drug design. Historical, Free-Wilson and Hansch approaches.
  • SAR in drug design.
  • The concept of isosterism. Bioisosterism as a tool in drug design.
  • Serendipity in drug design
  • Drug’s side effects in drug design
  • Random screening for biological activity
  • Application of hypothesis
  • Anti-metabolite approach to design a new drug.
  • Pro-drug/soft drug approaches to drug design
  • Drug Repurposing
  • Paradigms in drug discovery and development
  • Computational drug design: Chemoinformatics and bioinformatics: applications in drug design and development, molecular modeling, virtual screening, Docking, molecular dynamics, and Monte Carlos quantum methods, QSAR.