Medicinal Chemistry, CHM417/517, Spring 2008

TR 12:30 – 1:45 pm, Dobo 202

 

Course Policies and Syllabus

 

Instructor: Sridhar Varadarajan                 Office:                      229 Dobo Hall

Phone:          962-7350                                 Email:                       varadarajans@uncw.edu

Office Hours:         TR 1.45 pm – 3.00 pm, or by appointment.

Course Website: http://www.uncw.edu/chem/courses/varadarajan/chm417

UNCW email: You are required to frequently check your UNCW email account. Several announcements will be sent to this account throughout the semester. If you prefer to use some other email account, you can set up the UNCW account to forward all your email to your other account. Please contact ITSD if you need help.

 

Required Text: There is no required text for this course. Course materials and write-ups on certain topics will be posted periodically on the course website.

 

Reference Texts:  On reserve in the library. Can be borrowed for 4 hours at a time.

 

Several topics included in this course can be found in Foye's Principles of Medicinal Chemistry, 4th edition; David A. Williams, Thomas L. Lemke; Lippincott Williams & Wilkins: Philadelphia, 1995.

 

A couple of topics included in this course are covered well in Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry, 10th edition; Delgado & Remers, Eds.; Lippincott Williams & Wilkins: Philadelphia, 1998 ("W&G").

 

Support Texts: Any undergraduate organic and biochemistry texts.

 

Prerequisites:

 

CHM211 and CHM212. (A firm background in chemical principles and in the common functional groups of biological relevance will be required). Additionally, basic knowledge of the composition and functioning of eukaryotic cells will be required.

 

Goals:

 

The goal of this challenging course is to give the student an insight into the various principles involved in, and the multidisciplinary nature of, modern drug design. The course will focus on the chemical and biological principles that are fundamental to “medicinal chemistry”. Upon completion of the course the student should have a better understanding of how and why certain chemicals interact at biological targets.

           


The following is a tentative list of topics that shall be covered (not necessarily in this sequence):

 

Development and classification of drugs

Drug design and functional groups

Structure Activity Relationships

Physicochemical and Pharmacokinetics

Drug metabolism

Receptors and drug action

Drug design through Enzyme inhibition

Peptide and protein drugs

Drug action on DNA

 

Evaluation and Grading:

 

            There will be 3 exams and a final (worth 100 points each). The final will be a comprehensive exam, covering all course material. There will be no make-up exams. However, your score on any one of the first three exams will be replaced by your score on the finals, if it works to your benefit.

In addition, the class will be divided into groups of 5 students alphabetically and each group will submit a research paper, and give a 10 – 15 minute class presentation at the end of the semester, on any one biologically active organic compound currently being marketed as a drug (75 points). Each member of the team is required to email me the final write-up on his or her part of the research project.

Also, each student is required to submit 5 write-ups during the semester (5 points each) about current topics in the news, related to the course. Only one submission can be made in a single week. In other words, you cannot wait till the end of the semester and submit five write-ups in a single day!

  1. Each write-up should be submitted by email as WORD attachments.
  2. The subject of the email should only say “Submission # 1 (or 2, 3, 4, 5)”
  3. Each write-up should be no longer than 1 page in length (single spaced). It can be shorter.
  4. Each write-up should include a short descriptive title and the source of the topic (list the full reference including authors, publication, date, page numbers, etc. – no internet sources which are likely to disappear in a few weeks are acceptable).
  5. Each write-up should include a summary of the topic, a statement on how it relates to some topic you have learned in our class, and your personal opinion on the topic.

 

The maximum total points for the course is 500. Final grades will be assigned on the following percent scale: 90 – 100 = A; 80 – 89 = B; 70 – 79 = C; 60 – 69 = D; < 60 = F.

 

Important Dates:

 

Exams: Tu, 5th Feb, Th, 28th Feb, Tu 1st Apr. Finals: Th, May 1, 11.30 – 2.30pm

Selection of Research Topic: Th, Feb 9. Each team will select a topic and a team representative will submit it by email, along with the names of the team members and research assignments.

Team Meeting with Instructor: Before Spring Break. Each team will meet at least once with the instructor (during office hours, or by appointment if all team members are not free during office hours) to discuss progress of the research project.

Submission of Individual Research Report: Sat, Apr 5th.

Submission of Final Research Report: Th, Apr 10th.

Presentations: Apr 15, 17, 22, 24.

 

 

Research Report and Presentation:

 

            The topic (drug) will be decided by mutual agreement between the team members and the instructor. The following is a guideline for information that should be included (as applicable): Chemical Structure and physical properties, Discovery/Isolation/Synthesis, Company marketing the drug, Classification or therapeutic category, Mechanism of Action, Structure-Activity info, Method of Administration, Metabolism, Distribution, Elimination, Side Effects/Toxicity, etc.

            Information may be obtained from various news publications (newspapers, TIME, etc), scientific publications (Science, Science News, C&E News, Scientific American, Science Newsletter. etc), and journal articles (Journal of Medicinal Chemistry, Bioorganic and Medicinal Chemistry Letters, etc), drug manufacturer websites, pharmacy handouts, etc. Several journals are available online from campus, and can be accessed via the library web page.

           

The research report must be a formal typewritten report, with a title and list of authors, Introduction, Background, and all the sections suggested above, with all structures drawn using scientific software (ChemDraw, ChemWindows, etc), and all pages numbered. The report should be less than 10 pages long, and should include at least 5 literature references.

 

The final presentation should be made using Microsoft Powerpoint, should be 10 – 12 minutes long, and should focus on the topics of interest to the audience, and not on minor details. The presentation may be made either by one or more students from the team, however, questions may be addressed to any member of the team.

           

Class Attendance, Homework and Methods of Learning:

 

            Attendance at every lecture is expected though no formal attendance will be taken. Class attendance is invaluable to the learning process, and is highly recommended. If you must miss a lecture, it is your responsibility to obtain the materials distributed and the information provided during that class.

            Homework problems may be assigned in class, but will not be graded. Answers to the problems will be provided at a subsequent class. Students are strongly encouraged to discuss any difficulties they encounter with the instructor (and with classmates).

            The emphasis in this course is on learning and understanding the subject matter (though some memorization is unavoidable). You are likely to do better in the course by grasping the concepts rather than by memorizing topics. A good understanding of the principles explained in the earlier chapters will facilitate the learning of subsequent topics.

            Learning medicinal chemistry requires consistent effort and practice. As a rule, each lecture would require 2 – 3 hours of study outside class in order to achieve good grades. Sporadic bursts of study (just before exams) are very unlikely to yield good results.

            Often, announcements and information will be sent to your UNCW email accounts and posted on the course website. It is your responsibility to check your UNCW email and course website regularly.

 

Classroom Courtesy:

 

For the benefit of everyone in the class, all pagers and cellular phones must be turned off before entering the class. These devices are very disruptive to the entire class. It is your responsibility to notify anyone who might need to contact you during the class period (only in case of an emergency) that this can be done by contacting the Chemistry Department office at 962-3450. The message will then be relayed to you immediately by the office staff.

Students should be on time for class and stay for the entire class period. On the rare occasions when you may be delayed, I encourage you to come late rather than to miss class completely.

 

Academic Honesty:

 

            No form of dishonesty will be tolerated. Academic dishonesty takes many forms, from blatant acts of cheating to the more subtle forms of plagiarism, all of which are totally out of place in an institution of higher learning. Reporting and adjudication procedures have been developed to enforce the policy of academic integrity, to ensure justice, and to protect individual rights. Complete details may be found in the current Student Handbook and in the Code of Student Life.

 

UNCW practices a zero-tolerance policy for violence and harassment of any kind.  For emergencies contact UNCW CARE at 962-2273, Campus Police at 962-3184, or Wilmington Police at 911.  For University or community resources visit http://uncw.edu/wrc/crisis.htm.