COURSE INFORMATION
CHEMISTRY 3010/01
Fall Semester 2007
Tues, Thur 3:30 AM – 4:45 PM
MEDICINAL CHEMISTRY
3 credit hrs.
SC 212
INSTRUCTOR: Dr. Jennifer Powers, Science 429
Phone: (770) 423-6256
Email: jpowers@kennesaw.edu
Office Hours: M 9:30 -10:30 PM, W 1 – 2 PM, T Th 9:30-11 AM. Other hours by appointment
or any time you find me in my office. I am usually on campus all day Mon.-Fri.
PREREQUISITE: CHEM 3501 or 3500 (Biochemistry)
COURSE MATERIAL:
Lecture Textbook: An Introduction to Medicinal Chemistry, 3rd ed. by Graham L. Patrick.
Oxford University Press, 2005. ISBN 0-19-927500-9
WebCT Vista Access: Web CT will be utilized to post the syllabus, handouts, and class
notes/powerpoint slides. Announcements may also be made via WebCT. Please check this site
between classes. The web site is at http://vista.kennesaw.edu/ . If you do not know your
username and password necessary to log into Vista, you can click on the appropriate link when
you first go to that page. It is recommended that you change your password for security. An
alternate access site you may wish to bookmark is https://kennesaw.view.usg.edu
Student Email: KSU has a campus-wide email system. If you have not already setup your
account, go to http://netid.kennesaw.edu.
LEARNING OUTCOMES:
1. Describe the process of new drug approval in the United States.
2. To be able to use primary literature, databases, and internet and to obtain information about
drug development, mechanism of action and toxicity for a pharmaceutical agent.
3. To appreciate how drug development has changed through the years and have a basic
understanding of techniques commonly used today in drug design.
4. Classify the main biological targets of drugs and gives examples of the types of interactions
of drugs with their targets.
5. Explain the concept of structure-activity relationships, show common structural changes
made during drug discovery/development, and summarize types of physicochemical
parameters commonly used in SAR studies.
6. Explain why water solubility and lipid solubility are important factors related to drug
effectiveness and give examples of structural changes and formulations used to alter these
properties.
7. Define the processes of absorption, distribution, metabolism, and elimination; predict
common metabolites of drugs.
8. Understand that there are often many different biological targets one can choose for a
particular disease, and why drug specificity is hard to achieve.
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9. Have a molecular level understanding of the mechanism of action of several common classes
of drugs and be able to communicate this understanding either orally or in a written format.
10. To gain an appreciation of the interdisciplinary nature this field.
ATTENDANCE:
Regular lecture attendance is essential for success in this course. In the event that a student is
absent from a class, it is the student's responsibility to obtain missed information, hand-outs,
and announcements. In addition, attendance will be required on dates that we are doing
discussions or presentations. Attendance, on these dates only, is built into the participation
grade. If a student has a reasonable, documentable excuse for missing presentation days, talk
with the instructor to determine how your attendance will be counted.
All students will be expected to take the exams on the announced dates. If you are not physically
able to take an exam on the scheduled date, please see me to discuss how your grade will be
determined. You need to have documentation and a reasonable excuse to make up or be excused
from exams or attendance on required days.
LECTURE & EXAM PREPARATION:
There is a large volume of material to be learned in this course. Success in this course will
require much study out of class; students should expect to study a minimum of three hours out
of class for every one hour of lecture. It is not wise to fall behind in this course. To
encourage students to avoid cramming for exams, a short quiz will be given approximately 1
week prior to each exam.
In addition to reading/studying the assigned chapters and papers, students should study their
notes from class, assigned homework questions, and work through the multiple choice question
sets on-line for each assigned chapter. Assigned readings from journal articles will also be
considered part of the test material.
As with most chemistry courses, much of the later material builds on previous information. This
means you are expected to remember (and use) concepts learned the first several weeks
throughout the entire course!
GRADING:
Three Exams @ 18% each
Final Exam
Oral Presentation
Assignments/Participation/Quizzes
Grading Scale:
90 - 100%
80 - 89%
70 - 79%
60 - 69%
< 60%
54%
20%
13%
13%
A
B
C
D
F
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QUIZZES:
Short (10 -15 min) quizzes will be given on the dates listed in the schedule. Quizzes will be over
material that the student should have learned by that date (approximately 1 week before each
exam).
ASSIGNMENTS:
Assignments will include (1) reading and summarizing articles from the literature, (2) literature
search activities, and (3) a computer-based exercise. If an article is not available via a website, it
will be given as a handout or posted on Web CT. Due dates will be announced. Assignments
that are late will receive a lowered grade.
1.
2.
3.
4.
Finding drug information (handout and web-based searching)
Article summary – Drug Discovery
Article summary –Pharmacokinetics Issues
Docking exercise
PRESENTATIONS: You will work with one other person to become an “expert” regarding a
pharmaceutical agent of your choice. This should be chosen early in the semester, from a list
provided by the instructor, and you should locate and read papers during the semester. Various
due dates will be announced to ensure that progress is being made toward the presentation’s
completion; the student will lose points toward the presentation if due dates are not met. More
instructions on the oral presentation will be given later during the semester.
SUPPLEMENTAL MATERIAL: The textbook publishers have a companion website for this
book. It is at http://www.oup.com/uk/booksites/chemistry There you can find multiple choice
questions, 2D static structures, and 3D rotatable structures.
I have a few pharmacology and medicinal chemistry textbooks in my office. If anyone wishes to
check one of these out for an evening, please see me. There are also many supplemental sources
on the web. The NIH offers many helpful links for biochemistry, medicine, and pharmacology.
There are far too many sites to list, but here are a couple.
http://www.ncbi.nlm.nih.gov/Literature/index.html
http://www.nlm.nih.gov/medlineplus/druginformation.html
Others useful links include:
http://rxlist.com
http://www.fda.gov
http://www.medicinenet.com
http://www.centerwatch.com
http://www.chemweb.com/
All Modern Drug Discovery articles can be accessed for free: http://pubs.acs.org/journals/mdd/
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TENTATIVE COURSE SCHEDULE:
Note: This course assumes students have taken biochemistry and thus we will not be covering
Chapters 3 & 4 of this text. However, students are encouraged to review these chapters on their
own if they find it necessary.
Date
Aug 16
Aug 21
Topic
Introduction; Drugs & the Medicinal Chemist
The Why & The Wherefore: Drug Targets
Reading
Ch. 1
Ch. 2
Aug 23
Aug 28, 30
Sept 4
Sept 6, 11
Ch. 5
Ch. 9
Sept 13 (Th)
Proteins as Drug Targets: Receptors
Drug Design: Finding a Lead
Labor Day Holiday
Quiz 1
Drug Design: Optimizing Target Interactions
Case Study: ACE Inhibitors
EXAM 1
Sept 18
Sept 20, 25
Drug Development
Pharmacokinetics & Related Topics
Ch. 12
Ch. 8
Sept 27
Oct 2
Oct 4, 9
Drug Design: Optimizing Access to the Target
Quiz 2
Tools: QSAR, Combinatorial, Computers
Ch. 11
Oct 11 (Th)
Oct 16
Oct 18, 23
EXAM 2
Guest Speaker or Docking Exercise
Antibacterial agents
Oct 25
Review of Signal Transduction and Discussion
of Journal Articles
Anticancer Agents
Quiz 3
Cholinergics, Anticholinergics, and
Anticholineseterases
EXAM 3
Adrenergics
Oct 30, Nov 1
Nov 6, 8
Nov 13 (T)
Nov 15, 20
Nov 22
Nov 27, 29,
Dec 4
Thanksgiving Holidays begin—no class
Student Presentations
Dec 11 (T)
FINAL EXAM 3:30 PM – 5:30 PM
Ch. 10
Selected parts of Chs. 13,
14, 15
Ch. 16
Ch. 6
Ch. 18
Ch. 19
Ch. 20
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UNIVERSITY POLICIES:
NEW WITHDRAWAL POLICY: As of fall 2004, students will be allowed a maximum of eight total
withdrawals if they enter KSU as a freshman. Transfer students will be allowed one withdrawal per
fifteen credit hours attempted, for a maximum of eight. Students who choose to pursue a second degree at
KSU will be allowed two additional withdrawals. Students who entered KSU before the fall of 2004 will
be allowed one withdrawal per fifteen credit hours attempted for a maximum of eight.
To completely or partially withdraw from classes at KSU, a student must withdraw online at
http://www.kennesaw.edu, under Owl Express, Student Services. The date the withdrawal is submitted
online will be considered the official KSU withdrawal date which will be used in the calculation of any
tuition refund or refund to Federal student aid and/or HOPE scholarship programs. It is advisable to print
the final page of the withdrawal for your records. Withdrawals submitted online prior to midnight on the
last day to withdraw without academic penalty will receive a "W" grade. This does not affect the grade
point average. Withdrawals after midnight will receive a “WF”, which will be counted as an "F" in
calculation of their grade point average. Failure to complete the online withdrawal process will produce
no withdrawal from classes. Those students who stop attending classes and notify no one are usually
assigned failing grades which jeopardize their chances of future academic success. Call the Registrar's
Office at 770-423-6200 during business hours if assistance is needed.
The last day to withdraw without academic penalty is October 11. Failure to withdraw by the appropriate
date will mean that the student has elected to receive the final grades earned in the course. The only
exceptions to these withdrawal regulations will be for those instances which involve unusual and fully
documented circumstances.
Some general "fatherly" advice from the former Department Chair: "W" grades on your transcript
are a negative factor in evaluating your academic performance. Some professional schools go through a
transcript, substitute "F" for every "W", and recalculate the GPA. For all students, and especially for
anyone serious about a professional school of any kind, we would recommend that your transcript should
show no more than four "W" grades. Even if you have only four "W's" when you graduate, you should
have an excellent reason for each one of them (sickness, death in the family, etc.). Please take your
academic experience very seriously, and have a frank discussion with an advisor about your strengths and
weaknesses so that you do not waste time in an area where you are not likely to be successful. Your
teachers will do what they can to help all students succeed, but each student has to do their part in the
learning process.
ACADEMIC HONESTY: The policy on academic honesty is given in the college catalog and the
student handbook. It is summarized below. Students failing to adhere to this policy will be held
accountable. Cheating--in any form--is considered a serious offense and will be treated as such.
Academic Integrity Statement:
Every KSU student is responsible for upholding the provisions of the Student Code of Conduct, as
published in the Undergraduate and Graduate Catalogs. Section II of the Student Code of Conduct
addresses the University's policy on academic honesty, including provisions regarding plagiarism and
cheating, unauthorized access to University materials, misrepresentation/falsification of University
records or academic work, malicious removal, retention, or destruction of library materials,
malicious/intentional misuse of computer facilities and/or services, and misuse of student identification
cards. Incidents of alleged academic misconduct will be handled through the established procedures of
the University Judiciary Program, which includes either an “informal” resolution by a faculty member,
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resulting in a grade adjustment, or a formal hearing procedure, which may subject a student to the Code
of Conduct’s minimum one semester suspension requirement.
Suspicious behavior can get you in trouble. Keep your eyes on your own paper during Exams. Be
careful to prevent other students from seeing your paper during Exams.
Plagiarism: Copying or paraphrasing either all or a portion of another student’s homework,
assignments, or reports is improper and easily detected.
Disruption of Campus Life Statement: It is the purpose of the institution to provide a campus
environment, which encourages academic accomplishment, personal growth, and a spirit of understanding
and cooperation. An important part of maintaining such an environment is the commitment to protect the
health and safety of every member of the campus community. Belligerent, abusive, profane, threatening
and/or inappropriate behavior on the part of students is a violation of the Kennesaw State University
Student Conduct Regulations. Students who are found guilty of such misconduct may be subject to
immediate dismissal from the institution. In addition, these violations of state law may also be subject to
criminal action beyond the University disciplinary process.
Preview of Teaching Evaluation Questionnaire: The KSU faculty value student comments about the
course, instructor and materials, etc., which can be used to improve teaching and learning. A survey
consisting of the following questions will be distributed during the last two weeks of classes. Students
should consider them during the term and be prepared to answer them.
1. Identify the aspects of the course that most contributed to your learning (include examples of specific
materials, exercises and/or the faculty member’s approach to teaching, supervision and mentoring).
2. Identify the aspects of the course, if any,that might be improved (include examples of specific
materials, exercises and/or the faculty member’s approach to teaching, supervision and mentoring).
Suggested End-of Chapter Questions from Textbook
Ch. 2: 2-5, 7-10
Ch. 5: 1-8
Ch. 8: 1-9
Ch. 9: 1-3, 5
Ch. 10: 1-2, 4-10
Ch. 11: 3-9
Ch. 12: none
Ch. 13: 1-6
Ch. 16: 2-7
Ch. 18: 6-9
Ch. 19: 1, 3-9
Ch. 20: 3-5