R. Goennert
1961
Citations
1
Influential Citations
27
Citations
Journal
Bulletin of the World Health Organization
Abstract
In spite of the considerable amount of work on the chemotherapy of bilharziasis that has been carried out by numerous scientists, the treatment of schistosomal infections with drugs is still unsatisfactory. At the present time, two groups of compounds are mainly used for this purpose: the antimonials and the xanthones. The most widely used of the latter group is the thioxanthone " lucanthone ", commonly known by the trade names " Miracil D " (Bayer) and " Nilodin " (Burroughs Wellcome). Thousands of compounds belonging to different chemical groups have been screened, however, and some of them have proved to be effective in experimental Schistosoma mansoni infections, especially those of mice. The search for new drugs usually starts empirically. But experience has taught us the basic importance of the relationship between chemical constitution and biological activity in this kind of research. The continued discussion of this question may give valuable ideas to the investigator and may help finally to solve the problem. Our own investigations at the Institute are concerned mainly with Miracil D and its derivatives and with the application of experiences gained in regard to structure-activity relationship to other groups of compounds. This note briefly summarizes the results of our endeavours. By means of a technique developed by Kikuth & Gonnert a for infecting small mammals with S. mansoni (Liberian strain), during 1936-38 a large number of compounds from very different chemical groups was investigated for schistosomicidal activity. One of these substances, synthesized by Mauss b in 1938, showed a minor but convincing activity. This compound-l-N-f3-diethylamino-ethylamino4-methyl-xanthone-was later given the name "Miracil A" (Fig. 1). Further chemical and biological investigations have confirmed the hypothesis that the schistosomicidal activity of this chemical group depends on the