3806-42-6Relevant articles and documents
Synthesis, molecular modeling, selective aldose reductase inhibition and hypoglycemic activity of novel meglitinides
Salem, Manar G.,Abdel Aziz, Yasmine M.,Elewa, Marwa,Nafie, Mohamed S.,Elshihawy, Hosam A.,Said, Mohamed M.
, (2021/04/29)
In the present study, a novel generation of selective aldose reductase ALR2 inhibitors with significant hypoglycemic activities was designed and modulated based on rhodanine scaffold joined to an acetamide linker in between two lipophilic moieties. The synthesis of the novel compounds was accomplished throughout simple chemical pathways. Molecular docking was performed on B-cell membrane protein SUR1, aldehyde reductase ALR1 and aldose reductase ALR2 active sites. Compounds 10B, 11B, 12B, 15C, 16C, 26F and 27F displayed the highest hypoglycemic activities with 80.7, 85.2, 87, 82.3, 83.5, 81.4 and 85.3% reduction in blood glucose levels, respectively. They were more potent than the standard hypoglycemic agent repaglinide with 65.4% reduction in blood glucose level. Compounds 12B and 15C with IC50 0.29 and 0.35 μM were more potent than the standard ALR2 inhibitor epalrestat with IC50 0.40 μM. They were selective towards ALR2 over ALR1 134 and 116 folds, respectively. Molecular docking studies matched with the in-vitro and in-vivo results to elucidate the dual activities of both compounds 12B and 15C as potent antagonists for ALR2 over ALR1 and good agonists for the SUR1 protein.
New N-ribosides and N-mannosides of rhodanine derivatives with anticancer activity on leukemia cell line: Design, synthesis, DFT and molecular modelling studies
Awad, Mohamed K.,Elshaier, Yaseen A. M. M.,Gesson, Jean-Pierre,Khodair, Ahmed I.
, (2019/12/26)
N-ribosylation and N-mannosylation compounds have a great role in compounds activity as anticancer. The reaction of 2-thioxo-4-thiazolidinone (rhodanine) derivatives, as aglycon part, was done with ribofuranose and mannopyranose sugars (glycone part) foll
Studies on some thiazolidinones as antioxidants for local base oil
Mohammed, Hoda A.,Attia, Sayed K.,Nessim, Maher I.,Shaaban, Mohamed E.,El-Bassoussi, Ali A. M.
, p. 1619 - 1634 (2019/09/09)
In this work, 5 thiazolidinone derivatives of the type 5-benzylidene -2-(1-piperidinyl)-4-oxo-1,3-thiazolidine (101), 5-(4-butoxybenzylidene)-2-(1-piperidinyl)-4-oxo-1,3-thiazolidine (102), 5-(4-hexyloxybenzylidene)-2-(1-piperidinyl)-4-oxo-1,3-thiazolidine (103), 5-(4-octyloxybenzylidene)-2-(1-piperidinyl)-4-oxo-1,3-thiazolidine (104) and 5-(4-decyloxybenzylidene)-2-(1-piperidinyl)-4-oxo-1,3-thiazolidine (105) are synthesized and characterized using conventional tools analyses. They are tested as antioxidants for local base stock and the efficiency of these compounds, as antioxidants, was monitored through studying the change in total acid number and viscosity, the results reveal that the efficiency order is ranked as follows 105 > 104 > 103 >102 > 101. The quantum chemical parameters such as the lowest unoccupied molecular orbital (LUMO), the highest occupied molecular orbital (HOMO) energy levels and the energy gap (EHOMO-ELUMO) were calculated. The experimental results were on the same line with the quantum chemical calculations.
