119424-79-2Relevant academic research and scientific papers
Selenium analogs of phenoxypropionic and phenoxyacetic herbicides
Zakrzewski, Jerzy,Huras, Bogumi?a,Kie?czewska, Anna,Krawczyk, Maria
, p. 1005 - 1013 (2018/11/23)
Selenium analogs of phenoxyacetic herbicides, namely 2-(2,4-dichlorophenoxy)propionic acid (2,4-DP), 2-(2,4-dichlorophenoxy)acetic acid (2,4-D), 2-(4-chloro-2-methylphenoxy)propionic acid (MCPP), 2-(4-chloro-2-methylphenoxy)acetic acid (MCPA), 2-(2,4,5-trichlorophenoxy)propionic acid (2,4,5-TP), and 2-(2,4,5-trichlorophenoxy)acetic acid (2,4,5-T), were synthesized in two steps. Iodo aryl derivatives were dimerized with elemental selenium in the presence of CuO as catalyst to the corresponding diselenides. Diselenides were reduced with NaBH4 to a selenide anion and condensed with either propionic or chloroacetic acid to achieve the selenium analogs of phenoxyacetic herbicides. These selenium analogs show moderate herbicidal and fungistatic activity.
Synthesis and structure-activity relationships of novel phenoxyacetamide inhibitors of the Pseudomonas aeruginosa type III secretion system (T3SS)
Williams, John D.,Torhan, Matthew C.,Neelagiri, Venugopal R.,Brown, Carson,Bowlin, Nicholas O.,Di, Ming,McCarthy, Courtney T.,Aiello, Daniel,Peet, Norton P.,Bowlin, Terry L.,Moir, Donald T.
, p. 1027 - 1043 (2015/03/04)
The increasing prevalence of drug-resistant bacterial infections is driving the discovery and development not only of new antibiotics, but also of inhibitors of virulence factors that are crucial for in vivo pathogenicity. One such virulence factor is the type III secretion system (T3SS), which plays a critical role in the establishment and dissemination of Pseudomonas aeruginosa infections. We have recently described the discovery and characterization of a series of inhibitors of P. aeruginosa T3SS based on a phenoxyacetamide scaffold. To better characterize the factors involved in potent T3SS inhibition, we have conducted a systematic exploration of this structure, revealing several highly responsive structure-activity relationships indicative of interaction with a specific target. Most of the structural features contributing to potency were additive, and combination of those features produced optimized inhibitors with IC50 values 1 μM.
Pyrimidine derivatives
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, (2008/06/13)
Compounds of the formula STR1 wherein R1 is halogen, C1-4 -alkyl, halo-(C1-4 -alkyl) or C2-4 -alkanoyl, R2 is hydrogen, hydroxy, C1-4 alkoxy, C1-4 -alkylthio or phenyl-(C1-4 -alkoxy) or , when X is O, also acyloxy, R3 is hydrogen or C1-4 -alkyl, R4 is a carbocyclic group or a heterocyclic group, R5 is hydrogen or fluorine, m stands for zero, 1 or 2, X is O or NH and Y is a direct bond, --CH=CH--, --C C-- or a group of the formula of in which A is a C1-8 alkylene group which is optionally substituted by one or two phenyl groups, Z is O, S, SO or SO2 and n stands for zero or 1, with the proviso that R1 is different from iodine, when R2 is hydroxy or benzoyloxy, R3 is hydrogen, R4 is unsubstituted phenyl, R5 is hydrogen, m stands for zero, X is O, and Y is a direct bond, and tautomers thereof, which possess antiviral activity and can therefore be used in the form of medicaments for the control and prevention of viral infections are described. The compounds of formula I can be prepared according to known methods.
