16th International Symposium on Medicinal
Chemistry, 18-22 September 2000, Bologna, Italy
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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 symposiums 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 Clercqs 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.
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.
Main lectures and posters sessions were organized
around the following subjects:
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