14060-62-9Relevant academic research and scientific papers
Antiviral 2,5-disubstituted imidazo[4,5-c]pyridines: From anti-pestivirus to anti-hepatitis C virus activity
Puerstinger, Gerhard,Paeshuyse, Jan,De Clercq, Erik,Neyts, Johan
, p. 390 - 393 (2007/10/03)
A novel class of inhibitors of the hepatitis C virus [substituted 2-(2-fluorophenyl)-5H-imidazo[4,5-c]pyridines] is described. Introduction of a fluorine in position 2 of the 2-phenyl substituent of the lead anti-pestivirus compound 1 (5-[(4-bromophenyl)m
Metal-mediated inhibition of escherichia coli methionine aminopeptidase: Structure-activity relationships and development of a novel scoring function for metal-ligand interactions
Schiffmann, Rolf,Neugebauer, Alexander,Klein, Christian D.
, p. 511 - 522 (2007/10/03)
We report the discovery of thiabendazole as a potent inhibitor (K 1 = 0.4 μM) of Escherichia coli methionine aminopeptidase (ecMetAP) and the synthesis and pharmacological evaluation of thiabendazole congeners with activity in the upper nanomolar range, Elucidation of the X-ray structure of ecMetAP in complex with thiabendazole and an unrelated inhibitor that was independently described by another group showed that that both compounds bind to an additional CoII ion at the entrance of the active site. This unexpected finding explains the inactivity of the compounds under in vivo conditions. It also allows us to discuss the structure-activity relationships of this series of compounds in a meaningful way, based upon docking runs with an auxiliary metal ion, We describe a new scoring function for the evaluation of metal-mediated inhibitor binding that, unlike the previously used scoring function implemented in the docking program, allows us to distinguish between active and inactive compounds, Finally, conclusions for the structure-based design of in vivo-active inhibitors of ecMetAP are drawn.
VIRAL INHIBITORS
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Page 107, (2010/02/06)
The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine derivative having the general formula (Z): (formula). The invention als
SYNTHESIS AND PMR SPECTRA OF 2-HETARYL-SUBSTITUTED IMIDAZO-PYRIDINES AND IMIDAZOPYRIDINES
Yutilov, Yu. M.,Shcherbina, L. I.,Efremenko, A. F.
, p. 783 - 790 (2007/10/02)
A simple method for the synthesis of 2-hetarylimidazopyridines based on the oxidation with sulfur of a mixture of p-diaminopyridine and heterocyclic compounds that contain an active methyl group is proposed.The reaction of diamines with N-oxides of α- and
