p-Trifluoromethyl- and p-pentafluorothio-substituted curcuminoids of the 2,6-di[(E)-benzylidene)]cycloalkanone type: syntheses and activities against Leishmania major and Toxoplasma gondii parasites was written by Al Nasr, Ibrahim S.;Hanachi, Riadh;Said, Ridha B.;Rahali, Seyfeddine;Tangour, Bahoueddine;Abdelwahab, Siddig I.;Farasani, Abdullah;M. E. Taha, Manal;Bidwai, Anil;Koko, Waleed S.;Khan, Tariq A.;Schobert, Rainer;Biersack, Bernhard. And the article was included in Bioorganic Chemistry in 2021.Application of 33439-27-9 This article mentions the following:
A series of the title curcuminoids I (X = NH, NTs, S, CH2, etc.; R = CF3, SF5) with structural variance in the heteroatom of the cycloalkanone and the p-substituents of the Ph rings were tested for their activities against Leishmania major and Toxoplasma gondii parasites. The majority of them showed high activities against both parasite forms with EC50 values in the sub-micromolar concentration range. The compound I (X = NH; R = SF5) was not just noticeable antiparasitic, but also exhibited a considerable selectivity for L. major promastigotes over normal Vero cells. While derivatives differing only in the p-Ph substituents being CF3 or SF5 showed similar antiparasitic activities, the cyclic ketone hub was more decisive both for the anti-parasitic activities and the selectivities for the parasites vs. normal cells. QSAR calculations confirmed the observed structure-activity relations and suggested structural variations for a further improvement of the antiparasitic activity. Docking studies based on DFT calculations revealed L. major pteridine reductase 1 as a likely mol. target protein of the title compounds In the experiment, the researchers used many compounds, for example, 1-Tosylpiperidin-4-one (cas: 33439-27-9Application of 33439-27-9).
1-Tosylpiperidin-4-one (cas: 33439-27-9) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Application of 33439-27-9
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem