85002-36-4Relevant academic research and scientific papers
Synthesis, molecular docking, α-glucosidase inhibition, and antioxidant activity studies of novel benzimidazole derivatives
Singh, Gagandeep,Singh, Amanjot,Singh, Varinder,Verma, Raman K.,Tomar, Jyoti,Mall, Rajiv
, p. 1846 - 1866 (2020/08/03)
A novel series of N-methyl/benzyl-substituted benzimidazolyl-linked para-substituted benzyl-based compounds containing 2,4-thiazolidinediones, dimethyl malonate (DMM), and diethyl malonate (DEM) 17–27 were designed, docked, synthesized, and evaluated for their antidiabetic activity studies. Structures of all the synthesized compounds were confirmed through 1H NMR, 13C NMR, FTIR, and mass spectrometry. Four targeted compounds (17–18 and 22–23) showed good inhibitory potential in the range of 4.10 ± 0.01 to 9.12 ± 0.06 μM. Furthermore, synthesized compounds 17–27 were evaluated for their antioxidant potential and compared with standard ascorbic acid and results showed that compound 18 (EC50 = 0.176 ± 0.002 mM) being the most active. Compounds 17–18 and 22–23 exhibited prominent antidiabetic as well as antioxidant activity. Compound 18 was considered a promising candidate for this series. The designed molecules were docked into α-glucosidase protein (PDB Code. 3TOP) to develop a correlation with the α-glucosidase inhibition studies and were also additionally docked into PPARγ proteins (PDB ID: 2PRG) with rosiglitazone (standard drug) to study their PPARγ binding affinity in comparison with rosiglitazone and to classify these compounds for their PPARγ agonistic behavior.
Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor γ(PPARγ)
Hinnah, Konstantin,Willems, Sabine,Morstein, Johannes,Heering, Jan,Hartrampf, Felix W. W.,Broichhagen, Johannes,Leippe, Philipp,Merk, Daniel,Trauner, Dirk
, p. 10908 - 10920 (2020/11/09)
Photopharmacology aims at the optical control of protein activity using synthetic photoswitches. This approach has been recently expanded to nuclear hormone receptors with the introduction of "photohormones"for the retinoic acid receptor, farnesoid X rece
Design, synthesis and evaluation of novel thiazolidinedione derivatives as anti-hyperglycemic and anti-hyperlipidemic agents
Shrivastava, Sushant K.,Batham, Ankit,Sinha, Saurabh K,Parida, Tanmaya K.,Garabadu, Debapriya,Choubey, Priyanka K.
, p. 2258 - 2266 (2016/10/25)
A novel series of thiazolidine-2,4-diones was designed, synthesized and investigated for anti-diabetic activity. The (2,4-dioxo-1,3-thiazolidin-5-yl)methylphenylbenzamide derivatives contain an amide linkage between the central aryl ring and the hydrophobic tail. Structures of the compounds were confirmed by spectroscopic techniques fourier transform infrared spectroscopy, 1H-nuclear magnetic resonance and elemental (C, H, N) analysis. The synthesized compounds were evaluated for their in-vivo pharmacological activity (blood glucose and triglyceride lowering activity), where compounds thiazolidinediones-C and thiazolidinediones-E showed significant effects, comparable to the standard pioglitazone. Computational studies positively substantiated the nature and interaction of the designed compounds with peroxisome proliferator-activated receptor gamma.
Discovery of novel 5-benzylidenerhodanine and 5-benzylidenethiazolidine-2, 4-dione inhibitors of MurD ligase
Zidar, Nace,Toma?i?, Tihomir,?ink, Roman,Rupnik, Veronika,Kova?, Andreja,Turk, Samo,Patin, Delphine,Blanot, Didier,Contreras Martel, Carlos,Dessen, Andréa,Müller Premru, Manica,Zega, Anamarija,Gobec, Stanislav,Peterlin Ma?i?, Lucija,Kikelj, Danijel
supporting information; experimental part, p. 6584 - 6594 (2010/11/17)
We have designed, synthesized, and evaluated 5-benzylidenerhodanine-and 5-benzylidenethiazolidine-2,4-dione-based compounds as inhibitors of bacterial enzyme MurD with E. coli IC50 in the range 45-206 μM. The high-resolution crystal structure o
