Textbook (required): Delgado, J and Remers, W., "Textbook of Organic Medicinal and Pharmaceutical Chemistry," Lippincott-Raven, Philadelphia, 1998.

Suggested Support Texts: Undergraduate organic and biochemistry texts.

Ancillary reading: Various reading assignments will be assigned from the primary literature. My textbooks are available for overnight checkout. The Journal of Medicinal Chemistry should be viewed regularly.

Meeting time(s): There is one, three-hour lecture per week (with a break) on Tuesday from 2:00 - 5:00 and a weekly discussion section (1:00-2:00 Tuesdays; before class).

• Attendance: Do your best to make all the classes - we have only fourteen meetings scheduled!

• Course Aims. The aim of the class is to introduce graduate and upper level undergraduate students to the main theoretical concepts and experimental designs that support research in medicinal chemistry. Upon completion of this course, the student should have a better understanding of how and why certain chemicals interact at biological targets. The range of material will include: (a) folklore and herbal medicine practices, (b) metabolism, (c) physico-chemical and functional group properties or oragnic compounds, (d) lead compound identification, (e) empiric drug design, (f) modern computational drug design, and (g) select medicinal agents. The class content will be split; the first half of the semester will focus on the chemical and biochemical background needed to understand modern "medicinal chemistry" whereas the second portion of the semester will concentrate on the medicinal chemistry of select receptor-agent interactions. To help you through the course, I will make all lecture notes and structures available. This is not a memorization course - the emphasis is on understanding relationships between chemical structure and their individual mode of action.

• What I expect. (1) good attendance, (2) keeping up with reading assignments, (3) both good and bad feedback, (4) more than passive involvement and interest in the topics, (5) professional preparation and planning (don't wait till the last week to do your assignments) and (6) for chemistry students to better understand pharmaceutical sciences and for pharmaceutical sciences students to better understand chemistry.

• Grading. The letter grade will be assigned based upon performance in four areas: (a) a molecular modeling assignment (15%), (b) a research paper on a medicinally active agent (15%), (c) discussion group and journal club presentations (20%) and (d) three exams (total 50%; note that there is no final exam scheduled).

(a) molecular modeling assignment (due May 1st) - you will be asked to draw, minimize and examine the properties of a group of compounds using Tripos Software on the Silicon Graphics Workstation. In this exercise, you will learn how structural changes alter the properties of bioactive molecules. Topics assigned by instructor.

(b) research paper - a four-page (minimum) research paper on a medicinally important agent will be assigned. The content will include: (1) a graphical structure, (2) discovery/company, (3) brief review of the synthesis or preparation, (4) compound class and biological effects, (5) mode of action (how does it work), (6) significance, and (7) references. Research papers will be corrected, graded and returned to the student for revision. Upon revision, all papers will be photocopied, collated and distributed to all students in class.

(c) discussion group/journal club - the class will meet once weekly (in addition to the assigned class period) and discuss an article assigned from the Journal of Medicinal Chemistry or Bioorganic and Medicinal Chemistry Letters. One student will be selected to lead the discussion each week, however, everyone is responsible for understanding the article and contributing to the discussion. Our journal club will meet jointly with my research group.

(d) exams: three exams held on March 2, April 6, May 4). The exams will contain short answer, multiple choice, compare and contrast, etc., start at 4:10 and be approximately 45 minutes in length.