Medicinal Chemistry–iii. Main Lectures Presented At The Third International Symposium On Medicinal Chemistry

INTERNATIONAL UNION PURE A N D APPLIED OF CHEMISTRY ORGANIC CHEMISTRY DIVISION MEDICINAL CHEMISTRY—III Main lectures presented at the THIRD INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY held in Milan, Italy 13-15 September 1972 Symposium Editor P . PRATESI LONDON BUTTERWORTHS ENGLAND: B U T T E R W O R T H & CO. (PUBLISHERS) L T D . L O N D O N : 88 Kingsway, WC2B 6AB AUSTRALIA: B U T T E R W O R T H S PTY. L T D . S Y D N E Y : 586 Pacific Highway, Chatswood, N S W 2067 M E L B O U R N E : 343 Little Collins Street, 3000 B R I S B A N E : 240 Queen Street, 4000 CANADA: B U T T E R W O R T H & CO. ( C A N A D A ) L T D . T O R O N T O : 14 Curity Avenue, 374 NEW ZEALAND: BUTTERWORTHS OF NEW Z E A L A N D LTD. W E L L I N G T O N : 26-28 Waring Taylor Street, 1 SOUTH AFRICA: B U T T E R W O R T H & CO. ( S O U T H A F R I C A ) (PTY) L T D . D U R B A N : 152-154 Gale Street The contents of this book appear in Pure and Applied Chemistry, Vol. 35 N o . 4 (1973) Suggested U.D.C. number 54:61(063) 612015(063) © International Union of Pure and Applied Chemistry 1973 ISBN 0 408 70538 8 Printed in Great Britain by Page Bros (Norwich) Ltd, Norwich ORGANIZING COMMITTEE Chairman: P . PRATESI Secretary: A . SOLDI Treasurer: E . ADAMI Members : G . BERGAMI P . SENSI OPENING REMARKS PIETRO PRATESI Società Italiana di Scienze Farmaceutiche, Via Giorgio Jan, 18, Milan, Italy This international Symposium on Medicinal Chemistry, organized by the Società Italiana di Scienze Farmaceutiche, follows 10 years after the first Symposium, organized by the same Society in Florence, and 4 years after the Münster Symposium. All three Symposia have been sponsored by the International U n i o n of Pure a n d Applied Chemistry. T h e international chemical world's interest in Medicinal Chemistry is confirmed by the establishment, in 1970, of the Medicinal Chemistry Section of I U P A C . Medicinal chemistry has been defined as a basic science of health; and indeed it has m a n y facets, since it uses the theoretical a n d experimental means of all branches of chemistry, especially organic chemistry, physical chemistry a n d biological chemistry. F o r this reason each advance achieved in these branches of chemistry has a m a r k e d influence on medicinal chemistry, that is, on the latter's capacity to interpret the mechanism of action of drugs at the molecular level a n d to express qualitative a n d quantitative forecasts of the biological activity of substances. While many useful drugs are still discovered by semiempirical methods, I think it can nonetheless be asserted that recent advances in medicinal chemistry in the theoretical field allow a m o r e rational approach to drug design. The great successes achieved on the various frontiers of chemistry in the last few years a n d the increased degree of contact between chemistry and the biological sciences have certainly n o t been foreign to this result. It is for these reasons that the Organizers of this Symposium, in order to express the present trends in medicinal chemistry, have selected from a m o n g the most advanced topics some vivid examples of mutual cooperation among the basic sciences of medicinal chemistry. They felt that the main function of medicinal chemistry conferences is precisely to stimulate basic research in medicinal chemistry, to extend its frontiers a n d thus to encourage a better approach to therapeutic problems, in the interest of public hçalth. The scientific time-table of the Symposium is split into the following topics : (i) Biochemistry of microorganisms as a basis for the rational development of anti-infec