Medicinal Chemistry Course Descriptions


General Pharmaceutical & Inorganic 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, 1, 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 important.

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.

Pharmaceutical Inorganic Chemistry: 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.



General Physical, Organic and Radio Chemistry (2Units)                                    PMC 232

Physical Chemistry: 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. 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.

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.

Radiochemistry: Introduction to radiochemistry. Types, sources and measurements of radioactive particles. Biological effects of radiations. Photochemistry: general principles, characteristics of photochemical reactions and applications both in the synthesis and spoilage of drugs. Radio pharmacy: Pharmaceutical applications of radioisotopes and radiopharmaceuticals.

Applications of radiopharmacy: Examples of radiopharmaceuticals. Handling, dosing and disposal of radiopharmaceuticals. Pharmaceutical application of radio isotopes.

Practical Pharmaceutical Physical Chemistry (1Unit)                                           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.

Pharmaceutical Organic Chemistry (3 Units)                                                         PMC 331

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 memered 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 rotator dispersion and its uses. Importance of stereochemistry in terpenes.

Organic Synthesis on medicinal compounds involving several stages, e.g. preparation of benzocaine (Ethyl-p-aminobenzoate); Preparation of Aspirin; Preparation of sulphanilamide 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.

Pharmaceutical Specification and Standardization (2 Units)                                PMC 332

Official standards for pharmaceutical chemical 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: complexometric titrations, gravimetry and limit tests.

The sources of impurities in pharmaceutical products. Limit test to exclude excessive contamination, and Storage condition.

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, oxidation-reduction titrations.

Practical Pharmaceutical Qualitative Analysis (1Unit)                                          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; Cation analysis; Identification of acid radicals.

Instrumental Methods in Pharmaceutical Analysis (3 Units)                                PMC 431

Instrumental Methods for quantitative Analysis of pharmaceuticals: UV-

Visible spectrophotometry; Atomic Absorption spectroscopy, Flame photometry. Instrumental Methods for structure elucidation of drugs and natural products: Infra-red spectroscopy; 1D and 2D N.M.R. Spectrometry; Mass Spectrometry; Gas-liquid chromatography; HPLC, Hyphenated techniques like GC-MS, LC-MS and LC-NMR.

Medicinal Chemistry I (3 Units)                                                                               PMC432

A study of the following classes of drugs in respect of their nomenclature, physical and chemical properties, structure-activity relationship, synthesis (where necessary), assay, metabolism and uses: General and Local anaesthetics; Antidepressants; Antipsychotics; Anticonvulsants; Sedative-hypnotics; Analgesics, antipyretics and anti-inflammatory agents; Antihypertensive, diuretics, steroids including steroidal hormones.

Practical Pharmaceutical Analysis (1 unit)                                                 PMC 433

Experiments to cover volumetric and instrumental analysis of pharmaceuticals, which include: Determination of mixture containing borax and boric acid; Determination of the percentage of sodium salicylate and acetyl salicylic acid (Aspirin); Iodometric titration, Determination of ferrous and ferric ion in a mixture; Complexiometric titration using EDTA; Thin layer chromatography, Ultra-violet and visible spectrophotometry; NMR and MS spectra interpretation; Assay of calcium lactate tablet; Assay of sodium chloride in Dextrose/Saline.

Practical Pharmaceutical Synthesis (1 unit)                                                            PMC 435

Experiments to cover the synthesis of compounds of pharmaceutical importance, which include: Experiments on crystallization and melting points; Synthesis of aspirin; Synthesis of acetanilide; Synthesis of phenacetin; Synthesis of phenyl benzoate; Synthesis of m-dinitrobenzens; Synthesis of benzoin; Preparation of glucose from cane sugar; Preparation of caffeine from tea bags, Preparation of cysteine from hair; Preparation of oleoresins.

Pharmaceutical Analysis and Good Laboratory Principles (2 units)                   PMC531

Principles of good laboratory practice. Drug quality assurance system: Monographs and specification for drugs and drug products.

Analysis of drugs in biological samples. Applications of chemical and physicochemical analytical methods in purity determinations identification of pharmaceuticals, radio-pharmaceuticals and medicinal products;

Basic tests methodology for essential drugs. Equivalence and bioequivalence of drug products, biopharmaceutical methods in purity determination.

Other Instrumental Methods; e.g. Fluorimetry; Polarimetry, Polarography, Potentiometry.

Medicinal Chemistry, Drug Design and Development (3 Units)                           PMC532

Drug design: Physico-chemical approaches to drug design. Historical, Free-Wilson and Hansch approaches. The concept of isosterism. Bioisosterism as a tool in drug design. SAR in drug design. Anti-metabolite and pro-drug approach to design a new drug. Drug development: Stages in drug development. 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.

A study of the following classes of drugs in respect of their nomenclature, physical and chemical properties, structure-activity relationship, synthesis (where necessary), assay, metabolism and uses: chemotherapeutic agents such as antibiotics including sulphonamides, penicillins, cephalosporins, anti-malarials, anthelmintics, trypanocides, schistosomicides, amoebicides. Photochemistry, applications of radiopharmacy.