101494-92-2Relevant academic research and scientific papers
Synthesis and activity of 1H-benzimidazole and 1H-benzotriazole derivatives as inhibitors of Acanthamoeba castellanii
Kopańska, Katarzyna,Najda, Andzelika,Zebrowska, Justyna,Chomicz, Lidia,Piekarczyk, Janusz,Myjak, Przemys?aw,Bretner, Maria
, p. 2617 - 2624 (2007/10/03)
Chloro-, bromo- and methyl- analogues of 1H-benzimidazole and 1H-benzotriazole and their N-alkyl derivatives have been synthesized and tested in vitro against the protozoa Acanthamoeba castellanii. The results indicate that 5,6-dimethyl-1H-benzotriazole (11) and 5,6-dibromo-1H-benzotriazole (14) have higher efficacy than the antiprotozoal agent chlorohexidine.
Inhibitors of the NTPase/helicases of hepatitis C and related Flaviviridae viruses.
Bretner, Maria,Najda, Andzelika,Podwinska, Romualda,Baier, Andrea,Paruch, Katarzyna,Lipniacki, Andrzej,Piasek, Andrzej,Borowski, Peter,Kulikowski, Tadeusz
, p. 26 - 28 (2007/10/03)
Abstract: In the search for inhibitors of the non-structural protein 3 (NS3)-associated NTPase/helicase activities of the hepatitis C virus (HCV), and of the related West Nile Virus (WNV), and Japanese Encephalitis Virus (JEV), random screening of a broad range of unrelated low-molecular weight compounds revealed that 4,5,6,7-tetrabromo-1H-benzotriazole (TBBT) is a good inhibitor of the helicase activity of HCV and WNV NTPase/helicases (IC50 >> 20 mM and 1.7 mM with a DNA substrate), but a very weak inhibitor of the JEV enzyme (IC50 >> 200 mM). The synthesis of new TBBT derivatives was undertaken and their inhibitory activities against HCV, WNV, and JEV NTPase/helicases and cytotoxicities were examined. The N-alkyl derivatives showed good activity and lower cytotoxicity than TBBT.
