Inhibition of Trypanosoma cruzi Hexokinase by Bisphosphonates was written by Hudock, Michael P.;Sanz-Rodriguez, C. E.;Song, Yongcheng;Chan, Julian M. W.;Zhang, Yonghui;Odeh, Sarah;Kosztowski, Thomas;Leon-Rossell, Annette;Concepcion, J. L.;Yardley, Vanessa;Croft, Simon L.;Urbina, Julio A.;Oldfield, Eric. And the article was included in Journal of Medicinal Chemistry in 2006.Recommanded Product: 3-Bromophenyl acetate This article mentions the following:
Hexokinase is the first enzyme involved in glycolysis in most organisms, including the etiol. agents of Chagas disease (Trypanosoma cruzi) and African sleeping sickness (Trypanosoma brucei). The T. cruzi enzyme is unusual since, unlike the human enzyme, it is inhibited by inorganic diphosphate (PPi). Here, we show that non-hydrolyzable analogs of PPi, bisphosphonates, are potent inhibitors of T. cruzi hexokinase. We determined the activity of 42 bisphosphonates against TcHK, and the IC50 values were used to construct pharmacophore and comparative mol. similarity indexes anal. (CoMSIA) models for enzyme inhibition. Both models revealed the importance of electrostatic, hydrophobic, and steric interactions, and the IC50 values for 17 active compounds were predicted with an average error of 2.4à by using the CoMSIA models. The compound most active against T. cruzi hexokinase was found to have a 2.2 μM IC50 vs. the clin. relevant intracellular amastigote form of T. cruzi, but only a â?-2 mM IC50 vs. Dictyostelium discoideum and a human cell line, indicating selective activity vs. T. cruzi. In the experiment, the researchers used many compounds, for example, 3-Bromophenyl acetate (cas: 35065-86-2Recommanded Product: 3-Bromophenyl acetate).
3-Bromophenyl acetate (cas: 35065-86-2) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Recommanded Product: 3-Bromophenyl acetate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary