252758-93-3Relevant articles and documents
Synthesis, antifungal activity and QSAR of some novel carboxylic acid amides
Du, Shijie,Lu, Huizhe,Yang, Dongyan,Li, Hong,Gu, Xilin,Wan, Chuan,Jia, Changqing,Wang, Mian,Li, Xiuyun,Qin, Zhaohai
, p. 4071 - 4087 (2015/05/13)
A series of novel aromatic carboxylic acid amides were synthesized and tested for their activities against six phytopathogenic fungi by an in vitro mycelia growth inhibition assay. Most of them displayed moderate to good activity. Among them N-(2-(1H-indazol-1-yl)phenyl)-2-(trifluoromethyl)benzamide (3c) exhibited the highest antifungal activity against Pythium aphanidermatum (EC50 = 16.75 μg/mL) and Rhizoctonia solani (EC50 = 19.19 μg/mL), compared to the reference compound boscalid with EC50 values of 10.68 and 14.47 μg/mL, respectively. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were employed to develop a three-dimensional quantitative structure-activity relationship model for the activity of the compounds. In the molecular docking, a fluorine atom and the carbonyl oxygen atom of 3c formed hydrogen bonds toward the hydroxyl hydrogens of TYR58 and TRP173.
Potent 2′-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents
Patch, Raymond J.,Brandt, Benjamin M.,Asgari, Davoud,Baindur, Nand,Chadha, Naresh K.,Georgiadis, Taxiarchis,Cheung, Wing S.,Petrounia, Ioanna P.,Donatelli, Robert R.,Chaikin, Margery A.,Player, Mark R.
, p. 6070 - 6074 (2008/03/18)
A series of 2′-aminoanilides have been identified which exhibit potent and selective inhibitory activity against the cFMS tyrosine kinase. Initial SAR studies within this series are described which examine aroyl and amino group substitutions, as well as the introduction of hydrophilic substituents on the benzene core. Compound 47 inhibits the isolated enzyme (IC50 = 0.027 μM) and blocks CSF-1-induced proliferation of bone marrow-derived macrophages (IC50 = 0.11 μM) and as such, serves as a lead candidate for further optimization studies.
Amino (oxo) acetic acid protein tyrosine phosphatase inhibitors
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, (2008/06/13)
Compounds of formula (I) or therapeutically acceptable salts thereof, are protein tyrosine kinase PTP1B inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.