87545-48-0Relevant academic research and scientific papers
Further insights of selenium-containing analogues of WC-9 against Trypanosoma cruzi
Chao, María N.,Lorenzo-Ocampo, María V.,Szajnman, Sergio H.,Docampo, Roberto,Rodriguez, Juan B.
, p. 1350 - 1361 (2019/02/25)
As a continuation of our project aimed at searching for new chemotherapeutic agents against American trypanosomiasis (Chagas disease), new selenocyanate derivatives were designed, synthesized and biologically evaluated against the clinically more relevant dividing form of Trypanosoma cruzi, the etiologic agent of this illness. In addition, in order to establish the role of each part of the selenocyanate moiety, different derivatives, in which the selenium atom or the cyano group were absent, were conceived, synthesized and biologically evaluated. In addition, in order to study the optimal position of the terminal phenoxy group, new regioisomers of WC-9 were synthesized and evaluated against T. cruzi. Finally, the resolution of a racemic mixture of a very potent conformationally rigid analogue of WC-9 was accomplished and further tested as growth inhibitors of T. cruzi proliferation. The results provide further insight into the role of the selenocyanate group in its antiparasitic activity.
Optimization of 5-hydroxytryptamines as dual function inhibitors targeting phospholipase A2 and leukotriene A4 hydrolase
Meng, Hu,Liu, Ying,Zhai, Yujing,Lai, Luhua
, p. 160 - 167 (2013/03/13)
Dual function inhibitors targeting phospholipase A2 (PLA 2) and leukotriene A4 hydrolase (LTA4H) may balance the arachidonic acid (AA) metabolic network and be used as new anti-inflammatory drugs. In previous study, we discovered multi-target drugs towards the AA metabolic network, among which a dual-target inhibitor (JMC08-4) for human nonpancreatic secretory phospholipase A2 (hnps-PLA 2) and human leukotriene A4 hydrolase (LTA4H-h) was found. Based on the structure of compound JMC08-4, new dual-target inhibitors were designed assisted by molecular docking. In this report, a series of 5-hydroxytryptamine compounds were synthesized; and most of these title compounds showed more potent inhibitory activity than compound JMC08-4 in the in vitro bioassay against these two enzymes. The best one inhibited hnps-PLA 2 and LTA4H-h with IC50 values of 9.2 ± 0.5 μM and 2.4 ± 1.4 μM, respectively.
Activation and inhibition of leukotriene A4 hydrolase aminopeptidase activity by diphenyl ether and derivatives
Jiang, Xiaolu,Zhou, Lu,Wei, Dengguo,Meng, Hu,Liu, Ying,Lai, Luhua
scheme or table, p. 6549 - 6552 (2009/10/02)
The synthesis and biological evaluation of a series of diphenyl ether derivatives were described. The compounds can either activate or inhibit the aminopeptidase activity of leukotriene A4 hydrolase, while at the same time do not influence the
ARYL AMINO ACID DERIVATIVES AS INHIBITORS FOR TREATING INFLAMMATION
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Page/Page column 22, (2008/06/13)
The present invention relates to a chemical genus of 3-(triaryl)-2-aminopropanol derivative inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention of inflammatory diseases and disorders. The compounds have general formula III: A particular embodiment is
HETEROCYCLIC COMPOUNDS AS MODULATORS OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTORS, USEFUL FOR THE TREATMENT AND/OR PREVENTION OF DISORDERS MODULATED BY A PPAR
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Page/Page column 84, (2010/02/11)
The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
Oxime Ethers: New Potent Insect Growth Regulators
Ohsumi, Tadashi,Hatakoshi, Makoto,Kisida, Hirosi,Matsuo, Noritada,Nakayama, Isamu,Itaya, Nobushige
, p. 3197 - 3202 (2007/10/02)
Oxime ethers containing a 4-phenoxyphenoxy group in the molecules were synthesized and their insect growth regulating (IGR) activities were studied.Of these new IGR's, propionaldehyde oxime O-2-(4-phenoxyphenoxy)ethyl ether and propionaldehyde oxime O-2-(phenoxyphenoxy)propyl ether were found to be most effective, having much higher activities than methoprene against larvae of Culex pipiens pallens and Musca domestica by the immersion method and medium method, respectively.In addition, the effects of steric isomerism of these compounds were examined; their IGR activities were found to have a close relationship to the juvenile hormone activity by the Galleria wax test.
