Din, Zia Ud published the artcileSymmetrical and unsymmetrical substituted 2,5-diarylidene cyclohexanones as anti-parasitic compounds, Synthetic Route of 1205-17-0, the main research area is diarylidene cyclohexanone sym unsym preparation antiparasitic mol docking; 2,5-diarylidene cyclohexanones; Anti-parasitic; DFT analysis; Docking; T cruzi.
Sym. and unsym. bis-aryl-α,β-unsaturated ketones I (R = Ph, 4-MeOC6H4, 2-ClC6H4, etc.) and II [R1 = R2 = H, R3 = OMe, R4 = Ph, 4-MeNC6H4, 2,3-(MeO)2C6H3, 4-O2NC6H4, etc.; R1 = R2 = OMe, R3 = H, R4 = Ph, 4-BrC6H4, 2,6-Cl2C6H3, 2-MeO-4-O2NC6H3, etc.] were synthesized in moderate to excellent yield by treating cyclohexanone with various aldehydes. Dimethylammonium dimethylcarbamate (DIMCARB) was used as both catalyst and reaction medium for the synthesis of monoarylidenes cycloadduct intermediates, which were further used to produce diarylidene cyclohexanones. All 34 compounds synthesized were evaluated for their anti-proliferative activity, particularly against promastigote of Leishmania amazonensis, epimastigote and trypomastigote of Trypanosoma cruzi. Eighteen compounds displayed anti-leishmanial activity against promastigotes of L. amazonensis with IC50 values ranging from 2.8 to 10 μM. In addition, two compounds exhibited significant antitrypanosomal activity against epimastigotes of T. cruzi with IC50 values of 5.2±0.8 and 3.0±0.0μM, while five compounds exhibited activity from 15.0±1.4 to 30.2±1.8μM against trypomastigote of T. cruzi. Moreover, all compounds were more selective against the parasites than the epithelial cells. The unsym. compounds II [R1 = R2 = H, R3 = MeO, R4 = 2,3-(MeO)2C6H3; R1 = R2 = MeO, R3 = H, R4 = 4-O2NC6H4, 3,4,5-(MeO)3C6H2, 3,4-(MeO)2C6H3] can be considered as favorable anti-parasitic lead mols. having IC50 and EC50 values in the low-micromolar range, better than the reference drug benznidazole, and low cytotoxicity against Vero cells. The potent compounds were screened in silico against 17 enzymes of T. cruzi and the best scoring were found against Dihydroorotate Dehydrogenase.
European Journal of Medicinal Chemistry published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, Synthetic Route of 1205-17-0.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem