seco-Cyclothialidines: New Concise Synthesis, Inhibitory Activity toward Bacterial and Human DNA Topoisomerases, and Antibacterial Properties §

…, R Hanke, R Endermann, L Johannsen…

Index: Rudolph; Theis; Hanke; Endermann; Johannsen; Geschke Journal of Medicinal Chemistry, 2001 , vol. 44, # 4 p. 619 - 626

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Citation Number: 167

Abstract

seco-Cyclothialidines are a promising class of bacterial DNA gyrase B subunit inhibitors. A new seco-cyclothialidine derivative containing a dioxazine moiety, BAY 50-7952, was synthesized through a new concise pathway. One key step of the synthesis is the straightforward formation of the 2-aminothiazole derivative of S-tritylcysteine. In biological tests, BAY 50-7952 and other known seco-cyclothialidines exhibited high and selective ...

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