768-36-5Relevant academic research and scientific papers
SUBSTITUTED PYRAZ INYLMETHYL SULFONAMIDES FOR USE AS. FUNGICIDES
-
Page/Page column 55, (2009/10/22)
The present invention relates to the use of pyrazinylmethyl sulfonamides of formula (I) wherein Ra, n, R1, R2, R3, A, Y and D are as defined in the claims, and the N-oxides, and salts thereof for combating harmf
Synthesis, antimycobacterial and antifungal evaluation of 3-arylaminopyrazine-2,5-dicarbonitriles
Palek, Lukas,Dvorak, Jaroslav,Svobodova, Michaela,Buchta, Vladimir,Jampilek, Josef,Dolezal, Martin
, p. 61 - 65 (2008/12/20)
This paper describes preparation and biological evaluation of pyrazinamide analogues. Pyrazinamide with its simple structure gives a good opportunity for further modification regarding an increase of its antimycobacterial activity. We prepared a series of compounds derived from pyrazine-2,5-dicarbonitrile with arylamino substitution in position 3. All compounds were assayed in vitro against major Mycobacterium and various Fungi species. The best activity was found in 3-{[3-(trifluoromethyl)phenyl]amino}pyrazine-2,5-dicarbonitrile 11 with the value of 6.25 μmol-1 against M. tuberculosis H37Rv and moderate activity against minor Mycobacterium pathogens.
Metal-mediated inhibition of escherichia coli methionine aminopeptidase: Structure-activity relationships and development of a novel scoring function for metal-ligand interactions
Schiffmann, Rolf,Neugebauer, Alexander,Klein, Christian D.
, p. 511 - 522 (2007/10/03)
We report the discovery of thiabendazole as a potent inhibitor (K 1 = 0.4 μM) of Escherichia coli methionine aminopeptidase (ecMetAP) and the synthesis and pharmacological evaluation of thiabendazole congeners with activity in the upper nanomolar range, Elucidation of the X-ray structure of ecMetAP in complex with thiabendazole and an unrelated inhibitor that was independently described by another group showed that that both compounds bind to an additional CoII ion at the entrance of the active site. This unexpected finding explains the inactivity of the compounds under in vivo conditions. It also allows us to discuss the structure-activity relationships of this series of compounds in a meaningful way, based upon docking runs with an auxiliary metal ion, We describe a new scoring function for the evaluation of metal-mediated inhibitor binding that, unlike the previously used scoring function implemented in the docking program, allows us to distinguish between active and inactive compounds, Finally, conclusions for the structure-based design of in vivo-active inhibitors of ecMetAP are drawn.
Studies on Pyrazines. 18 . A New and Convenient Synthesis of 2-Amino-3-cyanopyrazine
Sato, Nobuhiro
, p. 817 - 819 (2007/10/02)
The titled compound, 2-amino-3-cyanopyrazine (1), was prepared by reaction of 3-aminopyrazine 1-oxide (7) with trimethylsilyl cyanide.Furthermore, conditions of individual steps in synthetic route to 7 starting from 2-pyrazinecarboxamide were optimized.
