《Mechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania》 was written by Medeiros, Andrea; Benitez, Diego; Korn, Ricarda S.; Ferreira, Vinicius C.; Barrera, Exequiel; Carrion, Federico; Pritsch, Otto; Pantano, Sergio; Kunick, Conrad; de Oliveira, Camila I.; Orban, Oliver C. F.; Comini, Marcelo A.. Safety of 2-BromoacetamideThis research focused ontrypanothione synthetase inhibition binding mode mol interaction Leishmania; Leishmania; Paullone; inhibition mode; thiol; trypanothione synthetase. The article conveys some information:
Trypanothione synthetase (TryS) produces N1,N8-bis(glutathionyl)spermidine (or trypanothione) at the expense of ATP. Trypanothione is a metabolite unique and essential for survival and drug-resistance of trypanosomatid parasites. In this study, we report the mechanistic and biol. characterization of optimized N5-substituted paullone analogs with anti-TryS activity. Several of the new derivatives retained submicromolar IC50 against leishmanial TryS. The binding mode to TryS of the most potent paullones has been revealed by means of kinetic, biophys. and mol. modeling approaches. A subset of analogs showed an improved potency (EC50 0.5-10μM) and selectivity (20-35) against the clin. relevant stage of Leishmania braziliensis (mucocutaneous leishmaniasis) and L. infantum (visceral leishmaniasis). For a selected derivative, the mode of action involved intracellular depletion of trypanothione. Our findings shed light on the mol. interaction of TryS with rationally designed inhibitors and disclose a new set of compounds with on-target activity against different Leishmania species. In addition to this study using 2-Bromoacetamide, there are many other studies that have used 2-Bromoacetamide(cas: 683-57-8Safety of 2-Bromoacetamide) was used in this study.
2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Safety of 2-Bromoacetamide
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