An article Novel 2,6-diketopiperazine-derived acetohydroxamic acids as promising anti-Trypanosoma brucei agents WOS:000482296400004 published article about DESIGN in [Fytas, George; Zoidis, Grigoris; Tsatsaroni, Alexandra; Tsotinis, Andrew] Univ Athens, Dept Pharmaceut Chem, Fac Pharm, Sch Hlth Sci, GR-15771 Athens, Greece; [Taylor, Martin C.; Kelly, John M.] London Sch Hyg & Trop Med, Dept Pathogen Mol Biol, Keppel St, London WC1E 7HT, England in 2019.0, Cited 15.0. Category: benzodioxans. The Name is 1-(4-Nitrophenyl)ethanone. Through research, I have a further understanding and discovery of 100-19-6
Aim: Identification of new, effective and selective trypanocidal agents. Materials & methods: Twelve novel acetohydroxamic acid derivatives based on 2-alkyl-2-aryl-2,6-diketopiperazine scaffolds have been synthesized and evaluated in vitro for their growth inhibitory activity against bloodstream form Trypanosoma brucei. Results: All the analogs were remarkably potent inhibitors, with low micromolar to submicromolar activities. Structure-activity relationship studies demonstrated that the presence of an alkyl substituent at the N(4)-position of the 2,6-diketopiperazine ring portion was, in general, beneficial to trypanocidal activity in this series. Conclusion: The highest activity resulted from the introduction of a methyl, n-propyl or n-butyl substituent to the N(4)-position of the parent compound. Importantly, the most potent analogs were found to be highly selective against T brucei with respect to mammalian cells. [GRAPHICS] .
Category: benzodioxans. About 1-(4-Nitrophenyl)ethanone, If you have any questions, you can contact Fytas, G; Zoidis, G; Taylor, MC; Kelly, JM; Tsatsaroni, A; Tsotinis, A or concate me.
Reference:
Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem