Miracil, ein neues Chemotherapeuticum gegen die Darmbilharziose

One Step Synthesis of N-[1-(2-Diethylamino-ethylamino)-7-(H or methoxy)-9-oxo-9H-thioxanthen-4-ylmethyl]-formamides and, Acetamide from Their Corresponding Alcohols, Hycanthone, and 7-Methoxy-hycanthone

“…Twenty-five milliliters of formamide was warmed to 140 C in an oil bath. 1 N-[1-(2-Diethylamino-ethylamino)-9-oxo-9H-thioxanthen-4-ylmethyl]acetamide (6). The mixture was stirred vigorously and 16 drops of sulfuric acid (0.21 mL, 4.01 mmol) in 6 mL of acetic acid was added.…”

“…Terms & Conditions of access and use can be found at http:// www.tandfonline.com/page/terms-and-conditions INTRODUCTION Lucanthone (Miracil D) (1) [1][2][3][4] and hycanthone (Etrenol) (2) [5][6][7][8] belong to the thioxanthenone class and have been well known as antischistosomal and anticancer agents. However, Taylor & Francis, our agents, and our licensors make no representations or warranties whatsoever as to the accuracy, completeness, or suitability for any purpose of the Content.…”

Milestones of helmintic research at Bayer

“…For this purpose, Kikuth started working with an experimental infection of a Liberian S. mansoni strain in mice in 1932; and, in 1938, this model was accomplished for screening studies by Kikuth and Go¨nnert. This was the first experimental model which had ever been started by a pharmaceutical company. As a result, a new schistosomicide, Miracil D, was developed (by Kikuth, Go¨nnert, Mauss) and patented in 1940 (Kikuth et al 1946;Du¨nschede 1971).…”

The Schistosomicidal Activity of Symmetrical Diaminodiphenoxyalkanes

“…After 1917, when tartar emetic was first used in the treatment of schistosomiasis (Christopherson, 1918), little advance was made in the development of schistosomicides until the lucanthone (miracil) series was synthesized by Mauss (1948). These were the first and only non-antimonial compounds shown to possess significant activity against Schistosoma mansoni in the mouse (Kikuth, Gonnert, and Mauss, 1946;Gonnert, 1947;Kikuth andGonnert, 1948, 1949).…”

“…These were the first and only non-antimonial compounds shown to possess significant activity against Schistosoma mansoni in the mouse (Kikuth, Gonnert, and Mauss, 1946;Gonnert, 1947;Kikuth andGonnert, 1948, 1949). They were inactive against S. japonicum in experimental animals (Vogel and Minning, 1948).…”