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Report from IUPAC-Sponsored Symposium

16th International Symposium on Medicinal Chemistry, 18-22 September 2000, Bologna, Italy

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Symposium website

It is the third time that this symposium was held in Italy (previously, it was held in Florence in 1974 and in Milan in 1978), but the Bologna location shed a unique light on the meeting. Bologna is the site of the oldest university in the world, as the University of Bologna was established almost a millennium ago in 1088. This noble locale demanded an outstanding effort of the Organizing Committee, chaired by Prof. C. Melchiorre (Uni versity of Bologna) to achieve a high standard for the scientific program. The symposium’s objectives were fully achieved, and 1 200 participants enjoyed a unique four-day event, merging scientific, cultural, and historical interests with world-famous Bolognese cuisine and well-known hospitality, along with the open-minded and fun-loving personality of the people of Bologna. The opening ceremony was initiated by Prof. Melchiorre, who introduced the symposium program to the audience, followed by representatives of IUPAC, the Medicinal Chemistry Division of the American Chemistry Society, the Asian Federation of Medicinal Chemistry, the European Federation of Medicinal Chemistry, and the Medicinal Chemistry Division of the Italian Chemical Society. All of these speakers further stressed the scientific and cultural attributes of the venue.

The prestigious Nauta Award for Medicinal Chemistry was given to Prof. E. De Clercq (Rega Institute for Medical Research, Katholieke Universiteit Leuven) for his outstanding work in antiviral research. Special mention is due De Clercq’s work in the HIV area, which he outlined in a plenary lecture. He reviewed all the potential mechanisms by which HIV could be targeted to provide new and effective therapies. For example, the replication of the virus could be stopped by reducing viral absorption to the cell by blocking it with polyanionic compounds containing the viral envelope glycoprotein, gp 120, which is instrumental to the adhesion process. Additional targets are the virus-cell fusion processes, blocked by certain oligopeptides, and viral assembly that could be prevented by dithiobisbenzamido derivatives. The importance of these newer approaches is further increased by the continuous appearance of HIV strains that are resistant to the current therapy.

> Ref.: E. De Clercq, Pure Appl. Chem. 73(1), 55-66 (2001)

The inaugural lecture on rational drug design was given by Prof. Daniel H. Rich (Department of Chemistry and School of Pharmacy, University of Wisconsin, Madison, Wisconsin, USA). What will it look like at the end of the 21 st century? After a historical overview on the progress made by medicinal chemists in the design and synthesis of new drugs, from the Erlich concept of the magic bullet to the use of computerized approaches, Prof. Rich suggested that the main limitation of effective drug design is our poor knowledge of the real conformations of protein receptors and enzymes. More powerful tools, such as understanding how certain natural toxins can easily cross barriers (i.e., the blood-brain barrier) will be available during the new century to help medicinal chemists overcome these issues. Prof. P. Krogsgaard-Larsen (Royal Danish School of Pharmacy, Copenhagen, Denmark) delivered a plenary lecture on inhibitory and excitatory amino acid agonists and antagonists and their potential application in the treatment of neurological disorders. Although the application of molecular biology to receptor classification has increased the number of receptor subtypes, chemical manipulation of prototype molecules has already produced a number of selective ligands that are able to interact with single subtypes. It is hoped that this development will result in more specific action of drugs that will eventually emerge from clinical trials.

Technology innovation is of paramount importance in current drug discovery process, as Dr. D. Trist (Glaxo Wellcome, Verona, Italy) outlined in his lecture. New technology, such as combinatorial chemistry and ultra-fast screening, have revolutionized the pace of new lead discovery, while the availability of genetic information from the human genome project will allow researchers to associate diseases with targets and validate them quickly. Lead compounds could be effectively optimized in terms of their physicochemical, pharmacokinetic, and toxicological properties, and then tested in humans to confirm their biological profile (proof of concept). In this way, the best molecules can be selected in the early phase of the discovery process, thereby greatly increasing the probability of success in the development phase.

> Ref.: E. Ratti and D. Trist, Pure Appl. Chem. 73(1), 67-75 (2001)

Main lectures and posters sessions were organized around the following subjects:

  • antihypertensive agents
  • impact of organic chemistry on drug discovery
  • antiinfective agents
  • hypolypidemics/antiatherosclerotics
  • anticancer agents
  • new paradigm in receptorology
  • natural products
  • antiviral agents
  • ligands for P1 and P2 receptors
  • neurodegenerative diseases
  • ligands for glutamate and GABA receptors
  • pain and inflammation

Presentations and posters were characterized by a high standard, with careful, detailed descriptions of the subjects treated. They sparked many stimulating scientific discussions.

Lastly, both the gala dinner and the concert represented wonderful highlights for this very successful symposium. The dinner took place at Villa Cicogna, a summer residence for Italian princes; it was built in 1570 by the renowned architect Jacopo Barozzi. More than 400 attendees at the dinner tasted the fantastic Bolognese food while viewing the magnificent frescoes. The concert was held in the Gothic Basilica of Santa Maria dei Servi, where about 800 attendees were entertained with a selection of classic pieces from Bach and Vivaldi to Verdi, all performed by a fine orchestra and choir.

Dr. Giovanni Gaviraghi
National Representative, IUPAC Medicinal Chemistry
Section Committee VII.M
Glaxo Wellcome S.p.A.
Medicines Research Center
Verona, Italy

> Published in Chem. Int. 23(3), 2001

> Two invited lectures published in Pure Appl. Chem. 73(1), 55-75 (2001)

> All lectures are published Il Farmaco Vol. 56, Nos 1-2, 2001

Page last modified 2 May 2001.
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