148433-00-5Relevant articles and documents
Synthesis of new symmetric cyclic and acyclic halocurcumin analogues typical precursors for hybridization
Noureddin, Sawsan A.,El-Shishtawy, Reda M.,Al-Footy, Khalid O.
, p. 5307 - 5323 (2020)
Abstract: It is believed that the synthesis of hybrid molecules containing different biologically relevant moieties would furnish multifunctional drugs with the possible synergism of potential importance for the treatment of cancer, diabetic and Alzheimer
1st generation dendrimeric antioxidants containing Meldrum's acid moieties as surface groups
Ai?pure, Klaudija,Jure, Māra,Mieri?a, Inese,Peipi?a, Elīna
, p. 607 - 620 (2022/01/22)
Free radical-caused oxidative stress can be reduced by various antioxidants. A new and promising type of antioxidant are monosubstituted Meldrum's acids. Herein the first dendritic architecture with 1,3-dioxane-4,6-dione units as surface groups is presented. The compounds were synthesized through the alkylation of phenol, the Knoevenagel condensation and sequential reduction. The antiradical activity (AA) against 1,1-diphenyl-2-picryl hydrazyl (DPPH) for all compounds is 80-90%, and the IC50 varies from 10-35 μM. These data are comparable with vitamin C, t-butylhydroquinone (TBHQ) or vitamin E. The AA against galvinoxyl (GO) increased with the number of surface groups. The AA was comparable with butylated hydroxytoluene (BHT) for compounds with at least two moieties of 1,3-dioxane-4,6-dione. The structure with a flexible glycerol core is highlighted among all the derivatives. Although the AA against DPPH for the glycerol derivative is comparable with those with aromatic cores it is more effective against GO (AA = 95%, IC50 = 60 μM): the AA is greater than for vitamin C and BHT. Thus, a flexible structure seems to be a promising core for elaborating powerful antioxidants with Meldrum's acid surface groups. This journal is
Synthesis of novel monocarbonyl curcuminoids, evaluation of their efficacy against MRSA, including ex vivo infection model and their mechanistic studies
Gagandeep,Kandi, Shamseer Kulangara,Kumar, Prince,Mukhopadhyay, Kasturi,Rawat, Diwan S.
, (2020/04/15)
In continuation of our effort to improve the physiological stability and the antibacterial activity of curcuminoids against drug-resistant bacteria, a series of novel monocarbonyl curcuminoids were synthesized and screened for antibacterial activity against S. aureus and E. coli strains. These curcuminoids showed potent antibacterial activity against both methicillin-sensitive and methicillin-resistant strains of S. aureus with MIC values 2–8 and 4–16 μg/mL, respectively. They also exhibited moderate potency against E. coli strains. The four most active curcuminoids (7d, 7i, 7m, and 7p) were on further investigation found to be very stable under physiological conditions, non-hemolytic, and non-toxic toward mammalian cells up to 150 μg/mL concentration. Mechanistic studies revealed that these curcuminoids displayed potent bactericidal activity by targeting cell membranes. Further, in an ex vivo mammalian co-culture infection model study, remarkably, the curcuminoids 7i and 7p were able to clear the internalized bacteria in mammalian cells and the activity was found to be superior to conventional antibiotics such as vancomycin and linezolid. Therefore, the present study affords us water-soluble, stable, non-toxic curcuminoids that may serve as lead molecules for development as antibacterial agents against MRSA infections.
