62001-31-4Relevant academic research and scientific papers
Novel TypeII Fatty Acid Biosynthesis (FAS II) Inhibitors as Multistage Antimalarial Agents
Schrader, Florian C.,Glinca, Serghei,Sattler, Julia M.,Dahse, Hans-Martin,Afanador, Gustavo A.,Prigge, Sean T.,Lanzer, Michael,Mueller, Ann-Kristin,Klebe, Gerhard,Schlitzer, Martin
, p. 442 - 461 (2013/08/25)
Malaria is a potentially fatal disease caused by Plasmodium parasites and poses a major medical risk in large parts of the world. The development of new, affordable antimalarial drugs is of vital importance as there are increasing reports of resistance to the currently available therapeutics. In addition, most of the current drugs used for chemoprophylaxis merely act on parasites already replicating in the blood. At this point, a patient might already be suffering from the symptoms associated with the disease and could additionally be infectious to an Anopheles mosquito. These insects act as a vector, subsequently spreading the disease to other humans. In order to cure not only malaria but prevent transmission as well, a drug must target both the blood- and pre-erythrocytic liver stages of the parasite. P.falciparum (Pf) enoyl acyl carrier protein (ACP) reductase (ENR) is a key enzyme of plasmodial typeII fatty acid biosynthesis (FASII). It has been shown to be essential for liver-stage development of Plasmodium berghei and is therefore qualified as a target for true causal chemoprophylaxis. Using virtual screening based on two crystal structures of PfENR, we identified a structurally novel class of FAS inhibitors. Subsequent chemical optimization yielded two compounds that are effective against multiple stages of the malaria parasite. These two most promising derivatives were found to inhibit blood-stage parasite growth with IC50 values of 1.7 and 3.0μM and lead to a more prominent developmental attenuation of liver-stage parasites than the gold-standard drug, primaquine.
Simple and convenient preparation of 1-(arylamino)methylbenzotriazoles and -(arylamino)methylbenzimidazoles
Milata,Kada,Zalibera,Belicova
, p. 215 - 220 (2007/10/03)
The preparation of 1-(arylamino)methylbenzotriazoles 1a-17a and benzimidazoles 1b-17b is described and their antibacterial activity evaluated. 1-Hydroxymethylbenzazoles react with the appropriate aniline to yield the target compounds. These were characterized using 1H NMR, IR, UV spectra. The compounds displayed no significant antibacterial activity.
Substituent effects in the bis(benzotriazolylmethylation) of aromatic amines
Katritzky, Alan R.,Rachwal, Stanislaw,Wu, Jing
, p. 446 - 455 (2007/10/02)
1-(Hydroxymethyl)benzotriazole and aromatic amines react to give an equilibrium mixture of N-mono- and N,N-bis(benzotriazolylmethyl)arylamines.Electron-releasing substituents on the arylamine ring shift the equilibrium towards the N,N-bis(benzotriazolylme
