| Instructor: | Dr. Salim M. Diab
Office: Room 215, St. Albert Phone: 815-740-3855 (Ext. 3855) Home Phone: 815-730-8302 E-mail: sdiab@stfrancis.edu homepage:http://www.stfrancis.edu/ns/diab/etherman.htm |
The course is held at the Morton Arboretum (Hwy 53) near Lyle, from 7:00-9:00 PM on Tuesday evenings.
Coordinators:
Douglas Armstrong, Olivet Nazarene University, Phone 815-939-5393,
FAX 815-939-5071, darmstrg@olivet.edu
Salim M. Diab, University of St. Francis, Phone 815-740-3855, FAX 815-740-4285,
SDiab@stfrancis.edu
Brent Friesen, Dominican University, jbfriesen@email.dom.edu
Schedule of topics, dates, and speakers:
Date
Topic
Speaker
Sept. 18 SAR by NMR: Discovering
Dr. Philip Hajduk, Abbott
High-Affinity Ligands for
Laboratories
Proteins
Sept. 25 Discovering New Drugs from
Dr. Doel Soejarto, College of
the Tropical Rain Forests in Pharmacy, University
of
the 21st Century: The UIC Illinois
at Chicago
ICBG Model
Oct. 2 A Molecular Tour
into the Dr. Jean Chmielewski,
Purdue
Design of HIV Therapeutics University
Oct. 9 1. Utility of
Fluorine in Biologically Dr. James McCarthy, Eli Lilly
Active Molecules, AND 2. The
Design and Synthesis of
Tezaciltabilne, a Mechanism-
Based Inhibitor of Ribonucleo-
tide Reductase
Oct. 16 Strategic Approaches for
the Dr. Steve Jacobsen,
Treatment of Alzheimer's
American Home Products,
Disease
Wyeth-Ayerst Research
Oct. 23 Effects of P-Glycoproteins
(P-gp) efflux on the brain deposition of two structurally related
neurokenin 1 (NK1) antagonists - by F. David Tingley III, Pfizer Global
Research and Development,
Pfizer, Inc.
Antimicrobacterial Agents for treatment of Tuberculosis and leprosy - by
Dr. Scott G. Franzblau, Director,
Institute For Tuberculosis Research, College of Pharmacy, UIC.
Oct. 30 Structure-based Drug Design
Dr. Jonathan Greer, Abbott
in Drug Discovery
Laboratories
Combinatorial Chemistry in the Dr. Thomas
J. Sowin,
Drug Discovery Process
Abbott Laboratories
Nov. 6 Radiopharmaceutical
Chemistry: Dr. Susan Z. Lever, MU
The Basics
Research Reactor, Univ.
of Missouri-Columbia
Nov. 13 The Role of Plants in Drug
Dr. Geoffrey A. Cordell,
Discovery: Past, Present, and College
of Pharmacy, Univ.
Future
of Illinois at Chicago
Required Texts:
None
References:
Journals
The following journals may be helpful to students taking this course.
1. Current Opinion in Pharmacology, a new (2001) review journal published
by Elsevier Science London.
2. Journal of Ethnopharmacology, edited by Dr. Doel Soejarto.
3. Journal of Medicinal Chemistry, published by the American Chemical
Society.
4. Journal of Medicinal Food, published by Mary Ann Liebert, Inc.
5. Journal of Natural Products, published by the American Chemical
Society and the American Society of Pharmacognosy.
6. Journal of Organic Chemistry, published by the American Chemical
Society.
7. Modern Drug Discovery, published by the American Chemical Society.
8. Molecular Pharmacology, published by the American Society of Pharmacology
and Experimental Therapeutics. (molpharm.aspetjournals.org)
9. Natural Product Reports, published by The Royal Society of Chemistry,
London, England.
10. Pharmaceutical Biology (formerly entitled International Journal
of Pharmacognosy).
11. Phytomedicine, published by Gustav Fischer Verlag, Stuttgart, Jena,
New York.
12. Trends in Pharmacological Sciences.
Specific Journal Articles
Listed below are just a few specific journal articles, which may be
of interest to students taking this course.
1. Trends in Pharmacological Sciences. For a review on pharmacologically
active marine natural products, see 1995, 16: 275-279.
2. "Chiral Drugs," Chemical and Engineering News, October 23, 2000,
pp. 55 ff.
3. "Chiral Chemistry," ibid., May 14, 2001, pp. 45 ff.
4. "Structure - Based Drug Design," ibid, June 4, 2001, pp. 69
ff.
5. "Buzzing About Potential Antimalarials," Modern Drug Discovery,
June, 2000, p. 13.
Books
The following books may be helpful to the students taking this course.
They are listed alphabetically by the last name of the (first) author or
editor.
1. "Supercritical Fluids: Extraction and Pollution Prevention," Edited
by Martin A. Abraham and Aydin A. Sunol, 1997, American Chemical Society,
ACS Symposium Series No. 670. This book includes supercritical fluid
extraction of natural products.
2. "Selective Toxicity: The Physico-chemical Basis of Therapy," Seventh
Edition, Adrien Albert, 1985, Chapman and Hall (London), ISBN 0-412-26010-7.
3. "Xenobiosis: Foods, Drugs, and Poisons in the Human Body," Adrien
Albert, 1987, Chapman and Hall (London), ISBN 0-412-28800-1 or 0-412-28810-9
(paperback).
4. "Drug Handbook -- A Nursing Process Approach," Rosalinda Alfaro
- LeFevre, Marcia E. Blicharz, Nancy M. Flynn, and Mary Jo Boyer, 1992,
Addison-Wesley Nursing, ISBN 0-201-09278-6.
5. "Plants, People, and Culture: The Science of Ethnobotany," Michael
J. Balick and Paul Alan Cox, 1997, Published by Scientific American
Library, Distributed by W.H. Freeman and Company, ISBN 1040-3213.
6. "Comprehensive Natural Products Chemistry," Editors -In-Chief, D.H.R.
Barton and K. Nakanishi; Executive Editor, O. Meth-Cohn, 1999,
Elsevier Science, ISBN 0-08-042709-X. This is a set consisting of
the following volumes:
Volume 1: "Polyketides and Other Secondary Metabolites Including
Fatty Acids and Their Derivatives."
Volume 2: "Isprenoids Including Carotenoids, and Steroids."
Volume 3: "Carbohydrates and their Derivatives Including Tannins,
Cellulose, and Related Lignins."
Volume 4: "Amino Acids, Peptides, Porphyrins and Alkaloids."
Volume 5: "Enzymes, Enzyme Mechanisms, Proteins, and Aspects
of NO Chemistry."
Volume 6: "Prebiotic Chemistry, Molecular Fossils, Nucleosides
and RNA."
Volume 7: "DNA and Aspects of Molecular Biology."
Volume 8: "Miscellaneous Natural Products."
7. "Nuclear Medicine Technology and Techniques," Third Edition, Edited
by Bernier, Christian, and Langan, 1994, Mosby, ISBN 0-8016-7060-8.
8. "Human Pharmacology," Second Edition, Theodore M. Brody, et al.,
1994, Mosby, ISBN 0-8016-7928-1.
9. "Pharmacognosy, Phytochemistry, Medicinal Plants," Jean Bruneton,
1995, Springer-Verlag, ISBN 1-898298-13-0.
10. "Pharmacology for Chemists," Joseph G. Cannon, 1999, American
Chemical Society, ISBN 0-8412-3524-4.
11. "Radiochemistry and Nuclear Chemistry," Second Edition, G. Choppin,
J. Rydberg, and J.O. Liljenzin, Butterworth Heimann, Ltd., 1995.
12. "Cutting's Handbook of Pharmacology," Seventh Edition, T.Z. Csaky
and Byron A. Barnes, 1984, Appleton-Century-Crofts, ISBN 0-8385-1418-9.
(NOTE: This book is out-of-print, so students will not be able to purchase
it, but might find it in a library. Also, a more recent name for
this publisher is Appleton-Lange.) 13. "Medicinal Chemistry Case
Study Workbook," Bruce Currie, Victoria F. Roche, and S. William Zito,
1996, Williams and Wilkins, ISBN 0-683-02260-1. As a case study,
this book poses various patient scenarios (i.e., patient has ____ symptoms,
or ____ disease, or ____ condition) and considers what should be done.
As such, this book represents an approach in which the emphasis is placed
on the patient, not on the drugs.
14. "Natural Products Medicine: A Scientific Guide to Foods/Drugs/Cosmetics,"
Ara Der Marderosian and Lawrence E. Liberti, 1988, George F. Stickley Company,
ISBN 0-89313-099-0.
15. "High Throughput Screening: The Discovery of Bioactive Substances,"
John P. Devlin, 1997, Dekker, ISBN 0-8247-0067-8.
16. "Medicinal Natural Products: A Biosynthetic Approach," Paul M.
Dewick, Wiley, 1997, ISBN 0-471-97478-1.
17. "Handbook of Medicinal Herbs," James A. Duke, 1987, CRC Press,
ISBN 0-8493-3630-9. This handbook catalogs 365 species of herbs having
medicinal or folk medicinal uses. Plants from all over the world,
from common cultivars to rare species, are included.
18. "Handbook of Edible Weeds," James A. Duke, 1992, CRC Press, ISBN
0-8493-4225-2. Although this book contains cautionary notes regarding
the potential allergenic or other harmful properties of many of the weeds,
it emphasizes finding practical uses for weeds, rather than waging pesticidal
war on them.
19. "Amazonian Ethnobotanical Dictionary," Edited by James Alan Duke
and Rodolfo Vasquez Martinez, 1994, CRC Press, ISBN 0-8493-3664-3.
This book was designed and conceived in the rainforest and is dedicated
to its preservation. Although this book places emphasis on plant
foods and rainforest medicines, there is also commentary on other relevant
applications, including natural pesticides. Dr. Richard E. Schultes,
Botanical Museum of Harvard University, internationally respected authority
in this area, commented about this book in Environmental Conservation as
follows: "We have waited a long time for this kind of listing of the natively
employed plants of the Amazonia. Here it is! And it will certainly
be a most useful compendium for every botanist, ethnobotanist, and anthropologist
who is working or intends to work in this most wonderful part of the world..."
20. "Principles and Practice of Nuclear Medicine," Second Edition,
Edited by P.J. Early and D. B. Sodee, 1995, Mosby, ISBN 0-8016-2577-7.
21. "Radiochemistry and Nuclear Methods of Analysis," William D. Ehmann
and Diane E. Vance, John Wiley and Sons, Inc., 1991.
22. "Trease and Evans Pharmacognosy," 14 th Edition, Evans, 1996, Saunders,
ISBN 0-7020-1899-6.
23. "Principles of Medicinal Chemistry," Fourth Edition, William O.
Foye, Thomas L. Lemke, and David A. Williams, Editors, 1995, Williams and
Wilkins, ISBN 0683033239.
24. "Medicinal Chemistry: The Role of Organic Chemistry in Drug Research,"
Second Edition, C.R. Ganellin and S.M. Roberts, Editors, 1993, Academic
Press, ISBN 0-12-274120-X.
25. "Phytochemical Diversity: A Source of New Industrial Products,"
Edited by M. Hayes, et al., 1997, The Royal Society of Chemistry, Special
Publication No. 200.
26. "Essentials of Nuclear Medicine Science," Edited by William Hladik,
III, Gopal Saha, and Kenneth Study, 1987, Williams and Wilkins, ISBN 0-683-04051-0.
27. "A Dictionary of Natural Products: Terms in the Field of Pharmacognosy
Relating to Natural Medicinal and Pharmaceutical Materials and the Plants,
Animals, and Minerals from Which They Are Derived," George M. Hocking,
1997, Plexus, ISBN 0-937548-31-6.
28. "Handbook of African Medicinal Plants," Maurice M. Iwu, 1993, CRC
Press, ISBN 0-8493-4266-X.
29. "Methods of Genome Analysis in Plants," Edited by Prem P. Jauhar,
1995, CRC Press, ISBN 0-8493-9437-6.
30. "Earthly Goods: Medicine-Hunting in the Rainforest," Christopher
Joyce, 1994, Little, ISBN 0-316-47408-8.
31. "Handbook of Ayurvedic Medicinal Plants," Edited by L.D. Kapoor,
1990, CRC Press, ISBN 0-8493-0559-4.
32. "Basic and Clinical Pharmacology," Eighth Edition, Edited by Bertram
G. Katzung, 2001, Lange Medical Books/McGraw-Hill, ISBN 0-8385-0598-8.
33. "Medicinal Chemistry: Principles and Practice," Frank D. King,
Editor, 1994, CRC Press, ISBN 0851864945.
34. "Human Medicinal Agents from Plants," Edited by A. Douglas Kinghorn
and Manual F. Balandrin, American Chemical Society Symposium Series 534,
1993, published by the American Chemical Society, Washington, D.C., ISBN
0-8412-2705-5.
35. "Essentials of Medicinal Chemistry," Second Edition, Andrejus Korolkovas,
1988, Wiley, ISBN 0-471-88356-5.
36. "Essentials of Molecular Pharmacology: Background for Drug Design,"
Andrejus Korolkovas, Reprint Edition, Books on Demand, Division of University
Microfilms International, Ann Arbor, MI, ISBN 0-317-07906-9.
37. "Radiopharmaceuticals in Nuclear Medicine Practice," Richard Kowalsky
and J. Randolph Perry, 1987, Appleton and Lange, ISBN 0-8385-8263-X.
38. "Phytomedicines of Europe: Chemistry and Biological Activity,"
edited by Larry D. Lawson and Rudolf Bauer, 1998, American Chemical Society,
ACS Symposium Series No. 691.
39. "Review of Organic Functional Groups: Introduction to Medicinal
Organic Chemistry," Third Edition, Thomas L. Lemke, 1992, Lea and Febiger,
ISBN 0-812-11428-0.
40. "Drugs and the Human Body -- With Implications for Society," Fourth
Edition, Ken Liska, 1994, Macmillian, ISBN 0-02-371091-8.
41. "Designing Bioactive Molecules: Three-Dimensional Techniques and
Applications," Edited by Yvonne Connolly Martin and Peter Willett, 1998,
American Chemical Society, ACS Professional Reference Books.
42. "Drug Actions, Basic Principles, Therapeutic Aspects," Ernst Mutschler,
et al., 1995, CRC Press, ISBN 0-8493-7774-9.
43. "Topics in Medicinal Chemistry: A Comprehensive Text for Students
and Practitioners in Health Sciences," Jay Nematollahi, 1983, Scientific
Service, No ISBN given.
44. "Medicinal Chemistry: A Biochemical Approach," Second Edition,
Thomas Nogrady, 1988, Oxford University Press, ISBN 0-19-505368-0 or 0-19-505369-9
for paperback.
45. "An Introduction to Medicinal Chemistry," Graham L. Patrick, 1995,
Oxford University Press, ISBN 0198558724 or 0198558716 for paperback.
46. "Anticancer Drugs from Animals, Plants, and Microorganisms," George
R. Pettit, et al., 1994, Wiley, ISBN 0-471-03657-9.
47. "Medicine Quest: In Search of Nature's Healing Secrets," Mark J.
Plotkin, 2000, Viking, ISBN 0-670-86937-6.
48. "Shaman's Apprentice," Mark J. Plotkin and Lynne Cherry, 1998,
HarBrace, ISBN 0-15-201281-8.
49. "Pharmacology," Third Edition, H.P. Rang and Gardner, 1995,
Churchill Livingstone, ISBN 0-443-07560-3.
50. "Pharmacology and Toxicology of Naturally Occurring Toxins," Edited
by H. Raskova, 1971, Pergamon Repr. UK, Franklin, ISBN 0-08-016797-7.
51. "Spices: Flavor Chemistry and Antioxidant Properties," Edited by
Sara J. Risch and Chi-Tang Ho, 1997, American Chemical Society, ACS Symposium
Series 660.
52. "Pharmacognosy and Pharmacobiotechnology," Robbers, Speedie, and
Tyler, 1996, Williams and Wilkins, ISBN 0-683-08500-X. This book
was written as a revision of the Ninth Edition of "Pharmacognosy," by Tyler,
Brady, and Robbers (see elsewhere in this list), but since it has a different
title, it is not the Tenth Edition.
53. "Natural and Synthetic Organic Medicinal Compounds," O. LeRoy Salerni,
1976, Mosby, ISBN 0-8016-4303-1. (Apparently this book is out-of-print,
so students will not be able to purchase it, but might find it in a library.)
54. "Top Drugs * Top Synthetic Routes," John Saunders, 2000, Oxford
University Press, ISBN 850100-5.
55. "The Organic Chemistry of Drug Design and Drug Action," Richard
B. Silverman, 1992, Academic Press, ISBN 0-12-643730-0. Dr. Timothy
Wilkinson used parts of this book in a medicinal chemistry course he taught
at Wheaton College.
56. "Flavours and Fragrances," Edited by K. Swift, 1998, The Royal
Society of Chemistry, Special Publication No. 214.
57. "Nursing Pharmacology -- An Integrated Approach to Drug Therapy
and Nursing Practice," Second Edition, Alvin K. Swonger and Myrtle P. Matejski,
1991, Lippincott, ISBN 0-397-54854-0.
58. "Chinese Drugs of Plant Origin: Chemistry, Pharmacology, and Use
in Traditional and Modern Medicine," W. Tang and G. Eisenbrand, 1992, Springer-Verlag,
ISBN 0-387-19309-X.
59. "Recent Developments in Flavour Science," Edited by A. Taylor and
D.S. Mottram, 1997, The Royal Society of Chemistry.
60. "Introductory Medicinal Chemistry," Second Edition, J.B. Taylor
and P.D. Kennewell, 1990, Prentice-Hall (United Kingdom), ISBN 0134988906.
61. "Bioactive Compounds from Marine Organisms: With Emphasis on the
Indian Ocean," Indo-United States Symposium, Edited by Mary-Frances Thompson,
et al., 1991, Published by A.A. Balkema NE, Ashgate Publishing Co., ISBN
90-6191-929-0.
62. "The Cross Name Index to Medicinal Plants," Anthony R. Torkelson,
1995, CRC Press. International in scope, this is a three-volume set,
providing over 4,000 scientific names, cross-indexed to more than 28,000
common names of medicinal plants. The first volume is organized alphabetically
by scientific name, whereas the other two volumes are a cross index by
common name.
ISBN for Volume 1: 0-849326311.
ISBN for Volume 2: 0-84932632X.
ISBN for Volume 3: 0-849326338.
ISBN for the whole set: 0-849326354.
63. "Hoosier Home Remedies," Varro E. Tyler, 1985, Purdue University
Press, ISBN 0-911198-77-6; paperback 0-911198-83-0.
64. "Honest Herbal: A Sensible Guide to the Use of Herbs and
Related Remedies," Third Edition, Varro E. Tyler, 1993, Haworth Press,
ISBN 1-56024-286-8; paperback 1-56024-287-6.
65. "Herbs of Choice: The Therapeutic Use of Phytomedicinals,"
Varro E. Tyler, 1994, Haworth Press, ISBN 1-56024-894-7; paperback 1-56024-895-5.
66. "Pharmacognosy," Ninth Edition, Tyler, Brady, and Robbers, 1988,
Lea and Febiger. ISBN 0-8121-11071-4.
67. "Principles of Nuclear Medicine," Second Edition, Edited by Wagner,
Szabo, and Buchanan, 1995, W. B. Saunders, ISBN 0-7216-9091-2.
68. "Economic and Medicinal Plant Research," Volume 6, Edited by H.
Wagner and Norman R. Farnsworth, 1994, Academic Press, ISBN 0-12-730067-8.
(There are also several other volumes.)
69. "The Practice of Medicinal Chemistry," Edited by Camille Georges
Wermuth, 1996, Academic Press, ISBN 0-12-744640-0.
70. "Herbal Drugs and Phytopharmaceuticals," Edited by Max Wichtl,
English edition translated and edited by Norman Grainger Bisset, 1995,
CRC Press, ISBN 0-8493-7192-9.
71. "Textbook of Organic Medicinal and Pharmaceutical Chemistry," Ninth
Edition, Charles O. Wilson and Ole Gisvold, 1991, Lippincott, ISBN 0-397-50877-8.
72. "Burger's Medicinal Chemistry and Drug Discovery," Fifth Edition,
Volume 2 -- "Therapeutic Agents," Manfred Wolff, Editor, 1996, Wiley, ISBN
0-471-575577.
73. "Burger's Medicinal Chemistry and Drug Discovery," Fifth Edition,
Volume 1 -- "Principles and Practice," Manfred Wolff, Editor, 1994, Wiley,
ISBN 0-471-575569.
74. "An Illustrated Chinese Materia Medica," Jing-Nuan Wu, 2001, ISBN
0-19-514017-6.
Publications Other than Journals and Books
The following items are very noteworthy, but do not fit into the categories
(journals, books) above.
1. "Annual Reports in Medicinal Chemistry," Volume 35, 2000, Academic
Press. See also earlier volumes, one per year, back to 1965.
2. "Advances in Medicinal Chemistry," started in 1992, published by
JAI Press.
3. "Progress in Medicinal Chemistry," started in 1961, published by
North-Holland Publishing Company and American Elsevier.
4. "The Pharmaceutical Century * Ten Decades of Drug Discovery."
Supplement to ACS Publications, 2000.
Web Links:
http://wings.buffalo.edu/academic/department/pharmacy/mch/public_html/informatic.html
http://www.weber.edu/ewalker/Medicinal_Chemistry/topoutline.htm
http://www.phc.vcu.edu/links.html
http://www.phc.vcu.edu/link/courses.html
http://pubs.acs.org/journals/jmcmar/index.html
http://www.chem.qmw.ac.uk/iupac/medchem/
http://www.aaps.org/
http://157.142.72.77/pharmacy/pharmint.html
http://www.rxlist.com/
http://monomerchem.com/display4.html
http://www.pharm.uu.nl/onderzk/medchem.html
http://dwb.unl.edu/Teacher/NSF/C01/C01Links/www.netaccess.on.ca/~dbc/cic_hamilton/med.html
http://members.tripod.com/~ChristopherMarrs/MedicinalChemistry.html
http://www.apnet.com/chemistry/journals.html
http://www.tripos.com/research/medchem.html
Expectations of Students:
1. Attendance is required. If you need to miss a lecture, please let
me know and we will work out a substitute assignment.
2. A feedback form is required for each speaker. The form will be distributed
on the day of the presentation and must be turned in to your instructor
the following week.
3. Active participation is encouraged. This can be done in the form
of questions, comments, or informal dialogue with the speakers and other
participants.
Criteria for Evaluation
One-hour credit: attend all lectures
and submit a written summary/critique of each lecture.
Two-hour credit: 50% of the grade
will be based on the same criteria as the one-hour credit. The other 50%
will be based on a research paper on one of the topics discussed in the
course. The paper must be 8-10 pages, well researched, properly cited with
all the relevant bibliography.