Graduate Medicinal Chemistry Course Descriptions
Medicinal Chemistry 501 - Principles of Medicinal Chemistry I: Drug Discovery Principles
This course focuses on the fundamental aspects and current methodologies involved in the drug discovery process. The fundamental aspects include the physical, chemical and pharmaceutical properties of drugs. The methodologies include lead discovery strategies, statistically based 2D and 3D QSAR optimization methods, structure-based and mechanism-based design methods, and combinatorial techniques. Application to the chemotherapy of cancer, viral and microbial diseases will be examined.
Medicinal Chemistry 502 - Principles of Medicinal Chemistry II
MCH 502 is a continuation of MCH 501. Drug metabolism, prodrugs and drug delivery systems are discussed in detail, as well as principles of pharmacokinetics and pharmacogenomics. In addition, prototypes of selected drug classes are discussed with a focus on the molecular mechanisms of action of representative drugs. Drug-target interactions at the molecular level will be examined using 3D-visualization techniques, which the students will learn to use. In this course, the medicinal chemistry topics are integrated with relevant topics in biochemistry, physiology, pharmaceutics, pharmacology and structural biology.
Medicinal Chemistry 514 - Protein & Peptide Chemistry
The class will discuss various topics on protein and peptide chemistry such as solid phase peptide synthesis, protein structure and design, peptide nucleic acids, peptoids, and betapeptides. Basic understanding of proteins will be provided as a foundation, followed by a discussion of recent papers focusing on the structure, function, and design aspects.
Medicinal Chemistry 515 - Structure Elucidation of Natural Products
A study of methods useful for the proof of structure of the alkaloids and other natural products.
Medicinal Chemistry 516 - Steroids
A study of the chemistry of steroids. The discussion will focus on interconversions, stereoselective syntheses, and structure-activity relationships of steroids, bile acids, D vitamins, and steroid hormones.
Medicinal Chemistry 517 - Heterocyclic Chemistry
The synthesis, reactions, and properties of 3-, 4-, 5-, and 6-membered heterocyclic rings will be discussed. The heterocyclic systems will include O, N, S, Se, and Te heteroatoms. Both pi-excessive and pi-deficient aromatic heterocycles will be described in the course as well non-aromatic analogues.
Medicinal Chemistry 518 - Active Site Chemistry
Chemical approaches to the design of specific inhibitors for labeling the active sites of enzymes.
Medicinal Chemistry 519 - Kinetics of Model Systems Related to Enzymic Reactions
Kinetics of model reactions related to biochemical reactions are studied. Implications from the results of model studies are applied to their biochemical counterparts with a view to rationalizing biochemical mechanisms using fundamental principles of organic chemistry.
Medicinal Chemistry 521 - Molecular Structure in Drug Design
A study of the development of quantitative methods useful for the correlation of biological activities with structural properties. Included are empirical de novo, linear free energy, and quantum statistical approaches.
Medicinal Chemistry 522 - Biosynthesis and Drug Metabolism
Discussion of the methods used in the study of the biosynthesis of selected natural products, in particular, terpenes, acetgenins, and aromatic compounds. Included is an introduction to drug metabolism and the significance of drug met
Medicinal Chemistry 524 - Mechanisms of Drug Action
This course reviews the general principles of drug action and the pharmacological activities of various classes of drugs. The major focus is on the molecular mechanisms of drug action, with a detailed discussion of one or more prototypes of each drug class. Selected examples of drug discovery and development are also discussed. At the completion of the course, students will have a knowledge of the molecular basis of pharmacological activity, the mode of action of major classes of therapeutic agents and be familiar with rational approaches to drug design utilizing mechanistic information.
Medicinal Chemistry 525 - Molecular Modeling
This course will focus on the current methods in structure-based design and the underlying physical science (e.g. what determines the binding free energy for a protein ligand). The lecture material will initially focus on the design of an individual ligand from the x-ray or NMR structure of the drug target protein (e.g. an enzyme) and subsequently will extend into designing libraries of ligands. There will be no textbook for the course but reading assignments will be given from the current literature, particularly review articles. The first half of the semester will be mainly formal lectures to give you the necessary background for doing subsequent hands-on modeling experiments. In the second half of the semester training sessions will be given on how to use the Tripos, Inc. Modeling software package SYBYL, and associated software modules, on our UB computer graphics workstations. You will then be given an independent modeling project wherein you will design a library of enzyme inhibitors based upon the structure of an enzyme. Upon completion of this course you will be able to independently carry out molecular modeling studies in support of drug design projects as well as use molecular modeling in support of bioorganic and organic chemistry research projects. Since a large selection of Tripos software and easily accessible computer graphics workstations are readily available to you at UB, you will be able to immediately put this new expertise to work in your graduate research projects when suitable; or use the expertise in your later research.
Medicinal Chemistry 527 - Combinatorial Chemistry
Combinatorial chemistry is a new field within the areas of medicinal/synthetic organic chemistry and chemical information technology. Most pharmaceutical and biotechnology companies have now incorporated combinatorial chemistry into their drug discovery research. Consequently, chemists/medicinal chemists with hands-on experience in this new technology are in high demand. Combinatorial chemistry centers on the design, simultaneous synthesis, and computerized tracking of many new compounds (i.e. “libraries” of compounds) in a highly efficient and automated fashion. This course will focus largely on the medicinal and synthetic organic chemistry aspects of combinatorial chemistry. The first third of the semester will be the lecture module of the course (1 credit) and the last two thirds will be the hands-on laboratory module of the course (2 credits). Students may take only the lecture module of the course, but the laboratory module requires achieving a grade of B- or better in the lecture module and prior approval from the instructor since the lab has limited enrollment. Equipment and supplies for the laboratory module are generously funded by the Camille & Henry Dreyfus Foundation Special Grant Program in the Chemical Sciences and by the University at Buffalo.
