- Synthesis and antimicrobial activity of novel substituted 4-[3-(1H-benzimidazol-2-yl)-4-hydroxybenzyl]-2-(1H-benzimidazol-2-yl)phenol derivatives
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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.
- Anil,Shankar,Bharath,Jalapathi
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p. 2648 - 2653
(2017/12/26)
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- Inhibitors of histone deacetylase
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The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
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Page/Page column 153
(2016/09/26)
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- Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity
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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.
- 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.
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p. 5543 - 5546
(2008/03/27)
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- INHIBITORS OF HISTONE DEACETYLASE
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The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
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Page/Page column 138-139
(2010/02/11)
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