50596-61-7Relevant academic research and scientific papers
Synthesis and metabolic studies of host-directed inhibitors for antiviral therapy
Moore, Terry W.,Sana, Kasinath,Yan, Dan,Krumm, Stefanie A.,Thepchatri, Pahk,Snyder, James P.,Marengo, Jose,Arrendale, Richard F.,Prussia, Andrew J.,Natchus, Michael G.,Liotta, Dennis C.,Plemper, Richard K.,Sun, Aiming
supporting information, p. 762 - 767 (2013/09/02)
Targeting host cell factors required for virus replication provides an alternative to targeting pathogen components and represents a promising approach to develop broad-spectrum antiviral therapeutics. High-throughput screening (HTS) identified two classes of inhibitors (2 and 3) with broad-spectrum antiviral activity against ortho- and paramyxoviruses including influenza A virus (IAV), measles virus (MeV), respiratory syncytial virus (RSV), and human parainfluenza virus type 3 (HPIV3). Hit-to-lead optimization delivered inhibitor 28a, with EC50 values of 0.88 and 0.81 μM against IAV strain WSN and MeV strain Edmonston, respectively. It was also found that compound 28a delivers good stability in human liver S9 fractions with a half-life of 165 min. These data establish 28a as a promising lead for antiviral therapy through a host-directed mechanism.
Regioselectivity of the reactions of 4,5-diphenylimidazole-2-thione with 1-chloro-2,3-epoxy-propane and 1-bromo-propene, efficient precursors for imidazo[2,1-b]thiazine and thiazole. Effect of microwave and solid support
Aouad, Mohamed R.,Rezki, Nadjet,El Ahsry, El Sayed H.
experimental part, p. 1321 - 1327 (2009/04/07)
(Chemical Equation Presented) A solid support under microwave (MW) irradiation without solvent allowed the synthesis of the 2,3-epoxy-propyl- thioimidazole 4, regioselectively, and prohibited its cyclization to give the imidazo[2,1-b]thiazine 3 from the r
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.
