849235-53-6Relevant articles and documents
Synthesis and antimicrobial activity of novel substituted 4-[3-(1H-benzimidazol-2-yl)-4-hydroxybenzyl]-2-(1H-benzimidazol-2-yl)phenol derivatives
Anil,Shankar,Bharath,Jalapathi
, p. 2648 - 2653 (2017/12/26)
A series of novel substituted bis-benzimidazole derivatives were synthesized by reaction of 5,5′-methylenebis(2-hydroxybenzaldehyde) with various substituted o-phenylenediamines in glacial acetic acid. The structure of the newly synthesized compounds was elucidated by 1H and 13C NMR, FT-IR, and MS spectra, and their antimicrobial activity against gram positive and gram negative bacteria and antifungal activity were evaluated. The thienyl-substituted derivative showed significant activity against Bacillus licheniformis. Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumonia (bacteria), and Fusarium solani (fungi). The activities of the fluoro-substituted substituted derivative against some bacterial strains and of the thienyl-substituted derivative against fungi were found to be similar to those of standard drugs.
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity
Moradei, Oscar M.,Mallais, Tammy C.,Frechette, Sylvie,Paquin, Isabelle,Tessier, Pierre E.,Leit, Silvana M.,Fournel, Marielle,Bonfils, Claire,Trachy-Bourget, Marie-Claude,Liu, Jianhong,Yan, Theresa P.,Lu, Ai-Hua,Rahil, Jubrail,Wang, James,Lefebvre, Sylvain,Li, Zuomei,Vaisburg, Arkadii F.,Besterman, Jeffrey M.
, p. 5543 - 5546 (2008/03/27)
Significant effort is being made to understand the role of HDAC isotypes in human cancer and to develop antitumor agents with better therapeutic windows. A part of this endeavor was the exploration of the 14 ? internal cavity adjacent to the enzyme catalytic site, which led to the design and synthesis of compound 4 with the unusual bis-(aryl)-type pharmacophore. SAR studies around this lead resulted in optimization to potent, selective, nonhydroxamic acid HDAC inhibitors.