41350-17-8Relevant academic research and scientific papers
Synthesis and evaluation as antitubercular agents of 5-arylethenyl and 5-(hetero)aryl-3-isoxazolecarboxylate
Vergelli, Claudia,Cilibrizzi, Agostino,Crocetti, Letizia,Graziano, Alessia,Dal Piaz, Vittorio,Wan, Baojie,Wang, Yuehong,Franzblau, Scott,Giovannoni, Maria Paola
, p. 162 - 172 (2013/05/22)
Preclinical Research A new series of 5-aryl and 5-arylethenylisoxazole carboxylate derivatives was synthesized and evaluated for in vitro activity against Mycobacterium tuberculosis H37Rv. Several compounds exhibited minimum inhibitory concentrations in the low micromolar range (2.3-11.4 μM). A variety of substituents introduced around the isoxazole ring allowed the delineation of preliminary SARs for this new series of compounds.
Fragment-based drug design and drug repositioning using multiple ligand simultaneous docking (MLSD): Identifying celecoxib and template compounds as novel inhibitors of signal transducer and activator of transcription 3 (STAT3)
Li, Huameng,Liu, Aiguo,Zhao, Zhenjiang,Xu, Yufang,Lin, Jiayuh,Jou, David,Li, Chenglong
supporting information; experimental part, p. 5592 - 5596 (2011/10/01)
We describe a novel method of drug discovery using MLSD and drug repositioning, with cancer target STAT3 being used as a test case. Multiple drug scaffolds were simultaneously docked into hot spots of STAT3 by MLSD, followed by tethering to generate virtual template compounds. Similarity search of virtual hits on drug database identified celecoxib as a novel inhibitor of STAT3. Furthermore, we designed two novel lead inhibitors based on one of the lead templates and celecoxib.
AZOLE CARBOXAMIDE INHIBITORS OF BACTERIAL TYPE III PROTEIN SECRETION SYSTEMS
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Page/Page column 80-81, (2010/02/14)
In accordance with the present invention, compounds of formula (I) that inhibit Type III protein secretion have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of Type III protein sec
Polyfunctional pyridines from nitroacetamidine and β-diketones. A useful synthesis of substituted imidazo[4,5-b]pyridines and related compounds
Batt,Houghton
, p. 963 - 969 (2007/10/02)
Nitroacetamidine undergoes a useful cyclocondensation with β-diketones to produce substituted 2-amino-3-nitropyridines. Use of an acylpyruvate generates hitherto unreported 2-amino-3-nitropyridine-4-carboxylates. These may be converted easily to functionalized imidazo[4,5-b]pyridines and oxazolo[5,4-b]pyridines.
