5653-60-1Relevant articles and documents
Development of Imidazoline-2-one Derivatives as Potential Antifungal and Anthelminthic Agents: in silico and in vitro Evaluation
Chilamakuru, Naresh Babu,Mallela, Vijaya Jyothi,Peraman, Ramalingam,Shaik, Shakir Basha,Simham, Venu,Singirisetty, Triveni
, p. 423 - 433 (2021/11/24)
Based on appropriate values of synthetic accessibility concerning from ADMET properties and docking scores by docking against proteins 3OZU and 1OJ0, a series of 4,5-diphenyl-1H-imidazol-2-ones (I1?15) were synthesized. The key intermediate, 2-hydroxy-1,2-disubstitutedethanones (E1?15) were prepared by benzoin condensation using 2:1 ratio of aromatic aldehydes and thiamine in the presence of alkali. Further, these cyclized ethanones (E1?15) were treated with urea to yield 4,5-diphenyl-1H-imidazol-2-one derivatives (I1?15) and were characterized by IR,1H NMR, Mass spectra, and CHNO analysis. The synthesized compounds were screened for their anthelmintic potential on Pheretima Posthuma along with standard albendazole, and antifungal activity (minimum inhibitory concentration method) on Candida albicans and Aspergillus niger along with standard miconazole. The results revealed that among all the tested compounds I3, I4, and I7 show considerable synthetic accessibility, docking scores, anthelminthic, and antifungal activity.
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives
Assadieskandar, Amir,Amini, Mohsen,Ostad, Seyed Nasser,Riazi, Gholam Hossein,Cheraghi-Shavi, Tayebe,Shafiei, Bentolhoda,Shafiee, Abbas
, p. 2703 - 2709 (2013/06/27)
A new series of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazoles were synthesized and their cytotoxic activities in vitro against four different cell lines (HT-29, MCF-7, NIH-3T3, AGS) were evaluated. Compound 6g bearing 3,4,5-trimethoxyphenyl moiety on ring A and 4-methoxy substituent on ring B displayed potent cytotoxic activity against all cell lines. Flow cytometry analysis and microtubule polymerization assay confirmed that cytotoxic activities of this compound were related to inhibitory effect against microtubules polymerization. Molecular modeling studies revealed that compound 6g could strongly bind to the colchicine binding site of α,β-tubulin through hydrogen bond interactions with Thrα179 and Cysβ241.
Discotic Liquid Crystals of Transition Metal Complexes 11: The First ?-Acceptor in Discotic Columnar Liquid Crystals Obtained from Octasubstituted Bis(diphenylethane-1,2-dithiolene)nickel Complexes
Ohta, Kazuchika,Hasebe, Hiroshi,Ema, Hiroshi,Moriya, Mitsuo,Fujimoto, Tetsuya,Yamamoto, Iwao
, p. 21 - 32 (2007/10/02)
Disk-like complexes, bisnickel (n-alkyl = n-hexyl, n-octyl) and bisnickel have been synthesized and characterized.It was found that n-decyloxy derivative exhibits a hexagonal discordered columnar (Dhd) mesophase while n-alkyl derivatives are not discotic liquid crystals but isotropic liquids at room temperature.The half-wave potentials for reduction of these complexes is -0.04 - -0.06 V. n-Decyloxy derivative is the first ?-acceptor in discotic columnar liquid crystals.