39908-69-5Relevant academic research and scientific papers
Synthesis and SAR study of 4,5-diaryl-1H-imidazole-2(3H)-thione derivatives, as potent 15-lipoxygenase inhibitors
Assadieskandar, Amir,Amini, Mohsen,Salehi, Marjan,Sadeghian, Hamid,Alimardani, Maliheh,Sakhteman, Amirhossein,Nadri, Hamid,Shafiee, Abbas
, p. 7160 - 7166 (2013/01/15)
A series of 4,5-diaryl-1H-imidazole-2(3H)-thione was synthesized and their inhibitory potency against soybean 15-lipoxygenase and free radical scavenging activities were determined. Compound 11 showed the best IC50 for 15-LOX inhibition (IC50 = 4.7 μM) and free radical scavenging activity (IC50 = 14 μM). Methylation of SH at C2 position of imidazole has dramatically decreased the 15-LOX inhibition and radical scavenging activity as it can be observed in the inactive compound 14 (IC50 >250 μM). Structure activity similarity (SAS) showed that the most important chemical modification in this series was methylation of SH group and Docking studies revealed a proper orientation for SH group towards Fe core of the 15-LOX active site. Therefore it was concluded that iron chelating could be a possible mechanism for enzyme inhibition in this series of compounds.
Acyl-CoA::cholesterol O-Acyl Transferase (ACAT) Inhibitors. 1. 2-(Alkylthio)-4,5-diphenyl-1H-imidazoles as Potent Inhibitors of ACAT
Harris, Neil V.,Smith, Christopher,Asthon, Michael J.,Bridge, Andrew W.,Bush, Raymond C.,et al.
, p. 4384 - 4392 (2007/10/02)
A potent, bioavailable ACAT inhibitor may have beneficial effects in the treatment of atherosclerosis by (i) reducing the absorption of dietary cholesterol, (ii) reducing the secretion of very low density lipoproteins into plasma from the liver, and (iii) preventing the transformation of arterial macrophages into foam cells.We have found that a mevalonate derivative 2, which contains a 4,5-diphenyl-1H-imidazol-2-yl moiety, inhibits rat hepatic microsomal ACAT in vitro and produces a significant hypocholesterolemic effect in the cholesterol-fed rat.Structure-activity relationships for analogues of 2 demonstrate that the 4,5-diphenyl-1H-imidazole moiety is a pharmacophore for inhibition of rat microsomal ACAT.
5,6-Diaryl-2,3-dihydroimidazothiazoles: A New Class of Immunoregulatory Antiinflammatory Agents
Bender, Paul E.,Hill, David T.,Offen, Priscilla H.,Razgaitis, Kazys,Lavanchy, Patricia,et al.
, p. 1169 - 1177 (2007/10/02)
A series of substituted 5,6-diaryl-2,3-dihydroimidazothiazoles were synthesized and evaluated in the rat adjuvant-induced arthritis and mouse oxazolone-induced contact sensitivity assays to determine the potential of these compounds for use as immu
Antiinflammatory agents, XVII: 4,5-Bis-(4-methoxyphenyl)-2-(arylthio)azoles with antiinflammatory activity
Klose,Niedballa,Schwarz,Bottcher
, p. 941 - 951 (2007/10/02)
The syntheses of 4,5-bis(4-methoxyphenyl)-2-(arylthio)imidazoles, -thiazoles and -oxazoles are described and their inflammatory activities are compared. Thioethers, sulfoxides, and sulfones of the phenyl, 4-fluorophenyl, and 2-thienyl derivatives were inv
5,6-Phenyl-2,3-dihydroimidazo [2,1-b] thiazoles
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, (2008/06/13)
The compounds are 5,6-phenyl-2,3-dihydroimidazo[2,1-b]thiazoles which have antiarthritic activity. A preferred compound is 5,6-bis(p-anisyl)-2,3-dihydroimidazo[2,1-b]thiazole.
