42445-05-6Relevant academic research and scientific papers
Vicinal diaryl azole-based urea derivatives as potential cholesterol lowering agents acting through inhibition of SOAT enzymes
Pal, Palash,Gandhi, Hardik P.,Kanhed, Ashish M.,Patel, Nirali R.,Mankadia, Niraj N.,Baldha, Satish N.,Barmade, Mahesh A.,Murumkar, Prashant R.,Yadav, Mange Ram
supporting information, p. 107 - 123 (2017/03/02)
A novel series of vicinal diaryl azole-urea derivatives were synthesized and evaluated for their potential to inhibit SOAT enzyme. Among the reported compounds, compound (12d) emerged as the most potent compound with an IC50value of 2.43?μM. In polaxamer-407 induced lipoprotein lipase inhibition model, compound (12d) reduced triglyceride turnover in?vivo. Compound (12d) also showed dose-dependent prevention of serum total cholesterol and prevention of LDL-C elevation at a dose of 30?mg/kg. Furthermore, compound (12d) showed potential to stop falling levels of serum HDL-C dose-dependently and improved the atherogenic index. Effect of 12d on body weight, plaque formation and development of atherogenic lesions were studied. Toxicological study of compound (12d) indicated that at a dose of 2000?mg/kg, 12d was devoid of any signs of toxicity or mortality.
Synthesis, cytotoxic evaluation, and molecular docking study of 4,5-diaryl-thiazole-2-thione analogs of combretastatin A-4 as microtubule-binding agents
Salehi, Marjan,Ostad, Seyed Nasser,Riazi, Gholam Hossein,Assadieskandar, Amir,Cheraghi-Shavi, Tayebeh,Shafiee, Abbas,Amini, Mohsen
, p. 1465 - 1473 (2014/03/21)
A series of combretastatin A-4 analogs in which cis-olefinic bond replaced by thiazole ring were prepared by reaction of α-bromo-1,2-(p-substituted) diaryl-1-ethanones and dithiocarbamate derivatives. The cytotoxicity of these compounds was determined against three cancer cell lines (HT-29), (MCF-7), (AGS) as well as fibroblastic cell line (NIH-3T3) using MTT assay. Inhibition of tubulin polymerization for some potent compounds was evaluated. These biological studies proved that 6j and 6o were the most potent compounds in this series. Furthermore 2-(methylthio)-substituted compounds show moderate or no activity. Docking studies involving 6j and 6o demonstrated that this analogs could be successfully docked in the colchicine binding site of α,β-tubulin.
Convenient and regiospecific method for synthesis of 4,5-diaryl-1-methyl-2- (methylthio)-1H-imidazole
Assadieskandar, Amir,Salehi, Marjan,Vosooghi, Mohsen,Shafiee, Abbas,Amini, Mohsen
, p. 2501 - 2507 (2013/07/25)
A convenient, high-yielding, regiospecific synthesis of 1H-imidazole-2-thiones ring has been developed. In addition, a series of 4,5-diaryl-1-methyl-2-(methylthio)-1H-imidazoles 8 were synthesized and characterized. The structure of regioisomers was confirmed through nuclear Overhauser effect spectroscopy and NMR spectroscopy. Copyright
UREIDE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
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Page/Page column 45, (2009/01/24)
This invention relates to a pharmaceutical comprising, as an active ingredient, a ureide derivative represented by formula: or a pharmaceutically acceptable salt thereof. The ureide derivative or a pharmaceutically acceptable salt thereof according to the present invention is useful for relieving pain and treating or preventing neuropathic pain.
COMPOUND FOR INHIBITING TYROSINE KINASE ACTIVITY OF DDR2 PROTEIN
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Page/Page column 28; 31, (2010/02/14)
A new furopyrimidine compound, their pharmaceutically acceptable salt, and a tyrosine kinase activity inhibitor. The furopyrimidine compound is a compound defined by chemical formula 1, 2, 3 or 4, on their precursor, and can exist as a form of free base or in an acid-addition salt. Since the furopyrimidine compound has an effect of inhibiting activity of DDR2 tyrosine kinase, it can be used in treating illnesses caused by the DDR2 tyrosine kinase activity such as hepatocirrhosis, rheumatoid arthritis or cancer.
Potential Hypolipidemic Agents: Part I-Synthesis and Hypolipidemic Activity of Some 4-(2,5-Substituted oxazole-4-yl)phenoxyalkanoic Acid Derivatives
Shridhar, D. R.,Ram, Bhagat,Sarma, C. R.,Saxena, N. K.
, p. 860 - 864 (2007/10/02)
A series of 4-(2-aryl-5-alkyl-aryloxazol-4-yl)phenoxyalkanoic acid derivatives (VI, 1-32) have been synthesised by O-alkylation of the corresponding 2-aryl-4-(4-hydroxyphenyl)-5-alkyl/aryloxazoles (Va-g) and evaluated for their hypolipidemic activity in rats of Wistar strain.Several compounds in this series show hypolipidemic activity comparable with that of the standard drug clofibrate at 200 mg/kg (p.o) dose.
