Design, synthesis and molecular docking studies of novel N-arylsulfonyl-benzimidazoles with anti Trypanosoma cruzi activity was written by Miana, Gisele E.;Ribone, Sergio R.;Vera, Domingo M. A.;Sanchez-Moreno, Manuel;Mazzieri, Maria R.;Quevedo, Mario A.. And the article was included in European Journal of Medicinal Chemistry in 2019.Application of 777-44-6 This article mentions the following:
In this report, we present the synthesis and biol. activity of 11 novel and 3 already reported N-arylsulfonyl-benzimidazole derivatives (NBSBZD, I [R1 = H, CH3], F etc. ) currently in development as potential anti-Tc compounds These compounds were designed as part of a library of synthetic arylsulfonyl heterocycle derivatives constructed from privileged structures exhibiting drug-like properties. Based on bioactivity assays against Tc, (in both the extracellular and intracellular forms), we observed that 10 compounds exhibited bioactivity against the epimastigote form, while six of them exhibited activity against the amastigote counterpart. Also, the compounds showed less cytotoxicity compared to the reference drug BZN as measured in Vero cell culture. In order to elucidate the potential mechanism of action, metabolite excretion profiles studies were performed, and complemented with mol. modeling studies performed over known Tc druggable targets. Consistency was observed between exptl. and theor. findings, with metabolic profiles showing that compounds I [R1 H, CF3, NHCOCH3; R2= R3 H, CH3, NO2; R4 = R5 H, CH3 ] interfered with the normal glycolysis cycle of Tc, while mol. modeling studies were able to establish a solid structure-activity relationship towards the inhibition of 6-phospho-1-fructokinase, a key enzyme involved in the parasite glycolytic cascade. Overall, the present study constitutes a multidisciplinary contribution to the development of new anti-Chagas compounds In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Application of 777-44-6).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Application of 777-44-6
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics