7087-65-2Relevant academic research and scientific papers
Pd-Catalyzed Decarboxylative Ortho-Halogenation of Aryl Carboxylic Acids with Sodium Halide NaX Using Carboxyl as a Traceless Directing Group
Fu, Zhengjiang,Jiang, Yongqing,Wang, Shuiliang,Song, Yuanyuan,Guo, Shengmei,Cai, Hu
supporting information, p. 3003 - 3007 (2019/05/10)
A highly regioselective Pd-catalyzed carboxyl directed decarboxylative ortho-C-H halogenation of cheap o-nitrobenzoic acids with NaX (X = I, Br) under aerobic conditions has been established. The utility of the method has been demonstrated by the gram-scale reaction and derivatization of the product. Experimental results have confirmed Pd and Bi played critical roles in the transformation and indicated the transformation might proceed via 2-halo-6-nitrobenzoic acid derivative intermediate.
STK4 INHIBITORS FOR TREATMENT OF HEMATOLOGIC MALIGNANCIES
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Paragraph 00704, (2017/01/09)
The application relates to compounds of Formula (I'): which modulate the activity of a kinase (e.g., STK4), a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease or disorder associated with the modulation of a kinase, such as STK4.
Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted- phenyl series
Alagille, David,Dacosta, Herve,Chen, Yelin,Hemstapat, Kamondanai,Rodriguez, Alice,Baldwin, Ronald M.,Conn, Jeffrey P.,Tamagnan, Gilles D.
supporting information; experimental part, p. 3243 - 3247 (2011/07/07)
We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl) ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl) ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.
Biologically selective potassium channel openers having 1,1- diethylpropyl group
Yoshiizumi, Kazuya,Seko, Norihiko,Nishimura, Noriyasu,Ikeda, Shoji,Yoshino, Kohichiro,Kondo, Hirosato,Tanizawa, Kazutaka
, p. 3397 - 3402 (2007/10/03)
To find out selective potassium channel openers (PCOs), we synthesized several 3,5-disubstituted phenylcyanoguanidine derivatives and investigated their structure-activity relationships (SAR). As a result, we discovered selective PCOs having 1,1-diethylpropyl group toward antihypertensive activity.
NMDA antagonists
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, (2008/06/13)
The present invention is directed to a new class of 4-sulfanimide-quinoline derivatives and to their use as NMDA antagonists.
Directed biosynthesis of 5'-fluoropactamycin in Streptomyces pactum
Adams,Rinehart
, p. 1456 - 1465 (2007/10/02)
A new pactamycin analogue, 5'-fluoropactamycin, was prepared by directed biosynthesis. Supplementation of the fermentation medium of Streptomyces pactum, var. pactum with 3-amino-5-fluorobenzoic acid, an analogue of 3-aminobenzoic acid, an advanced precursor in pactamycin biosynthesis, resulted in co-production of pactamycin and the new pactamycin analogue. A similar feeding experiment with 3-amino-5-methylbenzoic acid did not result in formation of the corresponding methylated pactamycin analogue, but only in inhibition of pactamycin production. Comparison of antimicrobial and cytotoxic activities of pactamycin and 5'-fluoropactamycin showed no significant differences.
Novel cyanoguanidine derivatives
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, (2008/06/13)
Compounds of the formula: STR1 wherein R1 and R2 are independently fluorine, chlorine or bromine atom, and R3 is a C4 -C7 alkyl having at least a branch at the C1 position, exhibit K+ channel opening activity and are useful as hypotensive agents and coronary vasodilators.
