SYLLABUS OF "FUNDAMENTALS OF DRUGS I", PHAR 331




1. Introduction and course overview (all instructors, 08/25).

I. DISCOVERY AND DEVELOPMENT OF SYNTHETIC AND NATURAL DRUGS (Cordell)

2. Modern drug discovery and the pharmaceutical industry (08/26).

3. Drugs of the future (08/27).
"ASSESSMENT" TEST, 2.30-3.30 PM., Tues. 08/26, Rm. 134-2 and 134-3

II. FUNCTIONAL CHEMISTRY OF PHARMACOPHORES AND BIOPOLYMERS(Kim)

4. Hybridization (08/28).

5. Structure, properties and nomenclature of functional groups found in biopolymers and drugs (09/02).

6. Structure of heteroarenes found in biopolymers and drugs (09/03).

7. General principles of acid-base chemistry (09/04).

8-9. Acid-base properties of functional groups found in biopolymers and drugs (heteroarenes and amino acids) (09/08-09/09).

10-11. Nucleophilic vs. electrophilic properties of functional groups found in biopolymers and drugs (09/10-09/11).
RECITATIONS, 1.30-3.30 PM., Tues.-Thur., 09/02-09/04 (Cordell and Kim) and 09/09-09/11 (Kim) (see section and TA assignment, 5th floor display case).

EXAM I (lectures 1-11), 2.30-3.30 PM., Thur., 09/18, Rm. 32 & 36, 150 pts

12. Chemical reactivity of ester, amide and acetal bond (09/15).

13-14. Specific reactions of heteroarenes and other functional groups (09/16-09/17).

15. Chemistry of phosphate group (09/18).

16. Chemistry of carbohydrates, oligo- and polysaccharides (09/22).

17. Combination of heteroarenes, glycosides and phosphate: nucleosides and nucleotides (09/23).

18. Reactivity of nucleic acids: hydrolysis, oxidation and alkylation of nucleic acid (09/24). REDOX CHEMISTRY (Bruzik)

19. Principles of REDOX systems (09/25).

20. Catalytic mechanisms of enzyme cofactors (09/29).
RECITATIONS, 1.30-3.30 PM. Tues.-Thur. 09/23-09/25 (Kim and Bruzik)

EXAM II (lectures 12-20), 2.30-3.30 PM., Thur., 10/09, Rm. 32 & 36, 150 pts

IV. STEREOCHEMISTRY (Bruzik)

21. Three point recognition (09/30).

22. Concepts and nomenclature of stereoisomerism, chirality and configuration (10/01).

23. Three dimensional shape of molecules: conformation (10/02).

24. Conformation of ester, amide, phosphate, and six-and five-membered ring systems (10/06).
RECITATIONS, 1.30-3.30 PM., Tues.-Thur., 09/30-10/02 (Bruzik)

V. NATURAL PRODUCTS (Kinghorn)

25. Introduction: Natural products from plants, microorganisms and marine sources (10/07).

26. Classification of natural product drugs: Alkaloids I (10/08).

27. Alkaloids II (10/09).

28 Isoprenoids (10/13).

29 Phenols and Quinones (10/14).

30. Introduction to phytopharmaceuticals (herbal remedies) (10/15).
RECITATIONS, 1.30-3.30 PM. , Tues.-Thur. 10/14-10/16 (Kinghorn)

MIDTERM, 2.30-3.30 PM. Thur., 10/23, Rm. 32 & 36, 200 pts

VI. NONCOVALENT INTERACTIONS AND BIOMOLECULAR STRUCTURE(Hopfinger)

31. Noncovalent interactions: hydrogen bonding, electrostatic interactions, hydrophobic effect (10/16).

32-33. Peptide and protein structure (10/20-10/21).

34. Nucleic acid structure (10/22).

35. Membrane structure (10/23).

36. Lipid-drug delivery systems (10/27).
RECITATIONS, 1.30-3.30 PM., Tues.-Thur., 09/28-09/30 (Hopfinger)

VII. CELL AND MOLECULAR BIOLOGY (lectures 37-43, Blond; lectures 44-46 & 54-58, Mankin; lectures 47-53, Neyfakh)

37. Cellular Structures: Classification of organisms. Prokaryotic and eukaryotic cell structure (10/28).

38. Membrane transport: Electrochemical potential. Active and passive transport (10/29).

39. Pumps. Na+/K+ ATPase. Ca2+ pumps. Ionophores (10/30).

40. Channels and pores. Ligand and voltage-gated channels. Nerve impulse (11/03)

41. Signal transduction cascades: Cell cycle. Vision (11/04).

42-43. Hormones and secondary messengers (11/05-11/06).
RECITATIONS, 1.30-3.30 PM., Tues.-Thur., 11/04-11/06, (Blond)

EXAM IV (lectures 31-40) 2.30-3.30 PM., Thur. 11/13, Rm. 32 & 36 (Hopfinger and Blond), 150 pts

44. Central dogma and genetic code: Principles of storage and expression of genetic information. Genetic code (11/10).

45. Replication and transcription. RNA processing and transport (11/11).

46. Protein synthesis. Ribosome. Inhibitors of translation (11/12).

47. Eukaryotic and bacterial genomes:Genome size. Introns. Gene families. "Junk DNA". Concept of "selfish DNA" (11/13).

48. Viruses: Viruses as autonomous genetic systems. Viruses as selfish DNA (11/17).

49. Autonomous genetic elements: Replication origin and telomers. Replication of bacterial and eukaryotic chromosomes. Plasmids. Recombination (11/18).
RECITATIONS, 1.30-3.30 PM. Tues.-Thur. 11/18-11/20 (Mankin and Neyfakh)

EXAM V (lectures 41-49), 2.30-3.30 PM., Tues., 11/25, Rm. 32 & 36 (Blond and Neyfakh) (Note the change of the exam day), 150 pts

50. Mechanisms of gene regulation: Operons. Positive and negative regulation of transcription (11/19).

51. Transcription factors. Enhancers. Regulation of translation (11/20).

52. Mechanisms of cell differentiation and development(11/24).

53. Cancer as a gene regulation disease (11/25).

54. Gene cloning: Enzymes used in gene cloning. Restriction enzymes. DNA ligase. DNA polymerase (11/26).

55. Plasmids and viruses as cloning vectors (12/01).

56. Transformation and selection of transformed cells. Gene libraries (12/02).

57. PCR: The principle of PCR method (12/03).

58. Application of PCR. Gene Cloning. Diagnostics. Forensics (12/04).
RECITATIONS, 1.30-3.30 PM., Tues.-Thur., 12/02-12/04, (Neyfakh and Mankin)

FINAL EXAM, time and date to be assigned by the College, 200 pts