210221-91-3Relevant academic research and scientific papers
Synthesis of (benzimidazol-2-yl)aniline derivatives as glycogen phosphorylase inhibitors
Galal, Shadia A.,Khattab, Muhammad,Andreadaki, Fotini,Chrysina, Evangelia D.,Praly, Jean-Pierre,Ragab, Fatma A.F.,El Diwani, Hoda I.
, p. 5423 - 5430 (2016)
A series of (benzimidazol-2-yl)-aniline (1) derivatives has been synthesized and evaluated as glycogen phosphorylase (GP) inhibitors. Kinetics studies revealed that compounds displaying a lateral heterocyclic residue with several heteroatoms (series 3 and 5) exhibited modest inhibitory properties with IC50values in the 400–600?μM range. Arylsulfonyl derivatives 7 (Ar: phenyl) and 9 (Ar: o-nitrophenyl) of 1 exhibited the highest activity (series 2) among the studied compounds (IC50324?μM and 357?μM, respectively) with stronger effect than the p-tolyl analogue 8.
Design and synthesis of three series of novel antitumor–azo derivatives
Lamie, Phoebe F.,Philoppes, John N.
, p. 1228 - 1240 (2017/05/04)
Three new series of thiazoles, quinolones, and thiazolidinones merged with benzimidazole, benzoxazole, and benzothiazole nuclei were synthesized. The compounds were subjected to Infrared, 1H nuclear magnetic resonance, 13C nuclear ma
Antiviral activity of benzimidazole derivatives. II. Antiviral activity of 2-phenylbenzimidazole derivatives
Tonelli, Michele,Simone, Matteo,Tasso, Bruno,Novelli, Federica,Boido, Vito,Sparatore, Fabio,Paglietti, Giuseppe,Pricl, Sabrina,Giliberti, Gabriele,Blois, Sylvain,Ibba, Cristina,Sanna, Giuseppina,Loddo, Roberta,La Colla, Paolo
scheme or table, p. 2937 - 2953 (2010/07/06)
Seventy-six 2-phenylbenzimidazole derivatives were synthesized and evaluated in cell-based assays for cytotoxicity and antiviral activity against a panel of 10 RNA and DNA viruses. The most commonly affected viruses were, in decreasing order, CVB-2, BVDV, Sb-1, HSV-1, and YFV, while HIV-1 and VSV were not affected, and RSV, VV and Reo-1 were only susceptible to a few compounds. Thirty-nine compounds exhibited high activity (EC50 = 0.1-10 μM) against at least one virus, and four of them were outstanding for their high and selective activity against VV (24, EC50 = 0.1 μM) and BVDV (50, 51, and 53 with EC50 = 1.5, 0.8, and 1.0 μM, respectively). The last compounds inhibited at low micromolar concentrations the NS5B RdRp of BVDV and also of HCV, the latter sharing structural similarity with the former. The considered compounds represent attractive leads for the development of antiviral agents against poxviruses, pestiviruses and even HCV, which are important human and veterinary pathogens.
Synthesis of some new benzimidazoles bearing different heterocyclic moieties. Part III
Mahmoud,El-Ezbawy,El-Sherief,Sarhan, Abd El-Wareth A. O.
, p. 1155 - 1163 (2007/10/03)
Interaction of 2-(p-aminophenyl)benzimidazole (I) with chloroacetyl chloride afforded N-chloroacetyl derivative II which was also obtained from the cycloaddition reaction of chloroacetyl chloride to the Shiff's bases V a-f. Reaction of II with mercaptans and/or secondary amines gave IIIa-c and IVa-c, respectively. Condensation of I with aromatic aldehydes afforded Shiff's bases V a-f, which on cyclocondensation with mercaptoacetic acid gave 4-thiazolidinones VI a-f. Reaction of I with substituted isothiocyantes furnished thiourea derivatives VIII a-c, which condensed with chloroacetic acid or its ester to form thiazolidinones IX a-c. Arylidines XI a-f were obtained from the reaction of IX a-b and aromatic aldehydes. Cyclization of VIII a-c with phenacyl bromide or bromoacetone afforded thiazoline derivatives XII a-k.
