Robert K Blackwood

Structure–Activity Relationships in the Tetracycline Series

Publisher Summary The tetracyclines may be defined as a family of broad-spectrum antibiotics, which have a perhydronaphthacene skeleton in common. Although discovered later than chlortetracycline and oxytetracycline, tetracycline is considered the parent compound for nomenclature purposes. In addition to these three tetracyclines, other tetracyclines that have found extensive clinical use are demethylchlortetracycline, rolitetracycline, methacycline, and doxycycline. Some common trade names and the typical oral and daily dosage of the tetracyclines are summarized in the chapter. The chapter discusses only the earliest stages of the route of a tetracycline from discovery to clinical use. This early stage is concerned with biological screening for in vitro and in vivo antibacterial activity. It is only at this level that a large number of derivatives have been studied so as to permit a detailed discussion of structure-activity relationships.