10149-57-2Relevant academic research and scientific papers
Synthesis and biological evaluation of trifluralin analogues as antileishmanial agents
Esteves,Fragiadaki,Lopes,Scoulica,Cruz
experimental part, p. 274 - 281 (2010/04/05)
A series of new analogues of trifluralin (TFL) were synthesized and characterized in view of changing the unfavorable properties that limits its use as antileishmanial agent. Some of the TFL analogues display more activity than a standard drug (miltefosine) against the promastigote forms of Leishmania infantum and Leishmania donovani and the intracellular form (THP-1 infected with L. infantum). All analogues showed a clear advantage over miltefosine, as they are not hemolytic. Some analogues can conjugate these characteristics with reduced cell toxicity and improved intracellular activity.
Kinetics of snar reactions of 1-phenoxy-nitrobenzenes with aliphatic amines in toluene: Ring substituent and solvent effects on reaction pathways
Isanbor, Chukwuemeka,Babatunde, Alice Ibitola
experimental part, p. 1078 - 1085 (2010/07/13)
Rate constants are reported for the reactions of a series of 4-substituted-1-phenoxy-2,6-dinitrobenzenes 1 and 6-substituted-1-phenoxy-2,4- dinitrobenzenes 2 activated by CF3, COOCH3, CN, NO 2 groups or by ring-nitrogen wi
Effects of ortho- and para-ring activation on the kinetics of S NAr reactions of 1-chloro-2-nitro- and 1-phenoxy-2-nitrobenzenes with aliphatic amines in acetonitrile
Crampton, Michael R.,Emokpae, Thomas A.,Isanbor, Chukwuemeka,Batsanov, Andrei S.,Howard, Judith A. K.,Mondal, Raju
, p. 1222 - 1230 (2007/10/03)
Rate constants are reported for reaction of 4-substituted 1-chloro-2,6-dinitrobenzenes 1, 6-substituted 1-chloro-2,4-dinitrobenzenes 2, and some of the corresponding 1-phenoxy derivatives, 3 and 4, with n-butylamine, pyrrolidine and pi-peridine in acetoni
Synthesis and evaluation of dinitroanilines for treatment of cryptosporidiosis
Benbow, John W.,Bernberg, Erin L.,Korda, Anna,Mead, Jan R.
, p. 339 - 343 (2007/10/03)
The efficacy of a series of dinitroaniline herbicide derivatives for the treatment of Cryptosporidium parvum infections has been studied. The lead compounds oryzalin (compound 1) and trifluralin (compound 2) have low water solubility (3 ppm) which was alleged to be a major contributor to their poor pharmacokinetic availability. Derivatives of compounds 1 and 2 were synthesized. In these derivatives the functionality at the C-1 amine position or the C-4 position was substituted with groups with various hydrophilicities to determine if a direct relation existed between water solubility and overall activity. The chlorinated precursors of these derivatives were also examined and were found to be less active in the C. parvum assays, a result in direct contrast to earlier work with Leishmania. Enhanced water solubility alone did not overcome the drug availability problem; however, several candidates with similar activities but with toxicities lower than those of the lead compounds were produced.
