Dedicated to Professor Rovfammet on the occasion of his 65th birthdayThe era of fi-lactam antibiotics, which represent the most important class of drugs against infectious diseases caused by bacteria, began more than fifty years ago with the discovery of penicillin G. Further improvements by isolation and structure elucidation of new natural compounds, and systematic chemical modification of these, is a striking example of to what extent chemistry can contribute to the progress of drug therapy. The complex relationship between structure and activity requires, even today, a largely empirical approach. The minimum structural unit for antibiotic activity had to be revised several times over decades. Both the activated b-lactam ring with an acidic group and the nature and spatial arrangement of the other substituents and rings decisively affect the potency, antibacterial spectrum, pharmacokinetics, and toxicity. Totally synthetic mono-and bicyclic compounds from the series of monobactams, penems, carbapenems, 1-oxacephems, and l-carbacephems are increasingly joining the classic groups obtained by semisynthesis from 6-aminopenicillanic acid and 7-aminocephalosporanic acid.
Mersacidin is a new peptide antibiotic of the proposed lantibiotic family. It is active in vitro and in vivo against Gram-positive bacteria including the methicillin-resistant Staphylococci. Its in vitro activity is less than those of vancomycin and erythromycin but it shows muchhigher activity in the in vivo system than can be expected from the in vitro testing results. A water soluble potassium salt has been prepared which has an activity profile similar to that of mersacidin, but has better in vivo activity against Streptococcus pyogenes than the parent compound.
A new glycopeptide antibiotic, balhimycin, has been isolated from the fermentation broth of a Amycolatopsis sp. Y-86,21022. Balhimycin belongs to the vancomycin class of glycopeptides and contains a dehydrovancosamine sugar. The biological activity of balhimycin has been compared extensively with that of vancomycin against methicillin resistant staphylococci and also against anaerobes. Balhimycin is marginally superior to vancomycin in its in vitro activity against anaerobes and in its bactericidal properties.
Professor Rolf Sammet zum 65. Geburtstag gewidmetVor mehr als 50 Jahren begann mit der Entdeckung von Penicillin G die Ara der P-LactamAntibiotica, die bis heute die wichtigste Wirkstoffklasse gegen bakterielle Infektionskrankheiten bilden. Die Weiterentwicklung durch Isolierung und Strukturaufklarung naturlicher Verbindungen und durch deren systematische chemische Abwandlung ist ein eindrucksvolles Beispiel dafiir, welchen Beitrag die Chemie zum Fortschritt der medikamentosen Therapie zu leisten vermag. Der komplizierte Zusammenhang zwischen Struktur und Wirksamkeit erfordert auch heute noch ein weitgehend empirisches Vorgehen. Die minimale strukturelle Einheit fur die Wirksamkeit muI3te im Laufe der Jahrzehnte mehrfach revidiert werden. Nicht nur der aktivierte 0-Lactamring rnit einer aciden Gruppe, sondern auch Natur und raumliche Anordnung der ubrigen Substituenten und Ringe beeinflussen entscheidend die Wirkungsstarke, Wirkungsbreite, Pharmakokinetik und Vertraglichkeit. Zu den klassischen Praparategruppen, die durch Partialsynthese aus 6-Aminopenicillansaure und 7-Aminocephalosporansaure gewonnen werden, gesellen sich zunehmend totalsynthetisch hergestellte mono-und bicyclische Verbindungen aus der Reihe der Monobactame, Peneme, Carbapeneme sowie I-Oxa-und l -Carbacepheme.
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