104097-35-0Relevant academic research and scientific papers
Biaryl-based anion receptors bearing thiourea groups: Fluoride anion receptor
Takahashi, Yohei,Endo, Masatoshi,Ito, Kazuaki
, p. 237 - 245 (2014/06/09)
The synthesis, characterization and binding studies with anions for biaryl-based anion receptors bearing thiourea groups have been described. The results revealed that receptors (1 and 2) showed good selectivity and binding affinity for F-, and among them binaphthyl-based receptor (1a) showed the best binding affinity for F-in comparison to other tested anions (Cl-, Br-, I-, NO-3 ; HSO-4 ; AcO-And H2PO-4 ). This is probably due to the fact that the moderate rigidity of binaphthyl skeleton in 1a is able to provide the better geometry of two thiourea groups for incorporating F-into the binding pocket. The higher basicity of F-Also participated in this selectivity. Springer Science+Business Media Dordrecht 2013.
Novel TypeII Fatty Acid Biosynthesis (FAS II) Inhibitors as Multistage Antimalarial Agents
Schrader, Florian C.,Glinca, Serghei,Sattler, Julia M.,Dahse, Hans-Martin,Afanador, Gustavo A.,Prigge, Sean T.,Lanzer, Michael,Mueller, Ann-Kristin,Klebe, Gerhard,Schlitzer, Martin
, p. 442 - 461 (2013/08/25)
Malaria is a potentially fatal disease caused by Plasmodium parasites and poses a major medical risk in large parts of the world. The development of new, affordable antimalarial drugs is of vital importance as there are increasing reports of resistance to the currently available therapeutics. In addition, most of the current drugs used for chemoprophylaxis merely act on parasites already replicating in the blood. At this point, a patient might already be suffering from the symptoms associated with the disease and could additionally be infectious to an Anopheles mosquito. These insects act as a vector, subsequently spreading the disease to other humans. In order to cure not only malaria but prevent transmission as well, a drug must target both the blood- and pre-erythrocytic liver stages of the parasite. P.falciparum (Pf) enoyl acyl carrier protein (ACP) reductase (ENR) is a key enzyme of plasmodial typeII fatty acid biosynthesis (FASII). It has been shown to be essential for liver-stage development of Plasmodium berghei and is therefore qualified as a target for true causal chemoprophylaxis. Using virtual screening based on two crystal structures of PfENR, we identified a structurally novel class of FAS inhibitors. Subsequent chemical optimization yielded two compounds that are effective against multiple stages of the malaria parasite. These two most promising derivatives were found to inhibit blood-stage parasite growth with IC50 values of 1.7 and 3.0μM and lead to a more prominent developmental attenuation of liver-stage parasites than the gold-standard drug, primaquine.
Cytosine analogues from substituted acetonitriles via Thorpe condensation
Barkin, Julia L.,Faust Jr., Marcus D.,Trenkle, William C.
, p. 3333 - 3335 (2007/10/03)
(Matrix presented) A Thorpe condensation is the key bond construction in a rapid and efficient synthesis of substituted cytosine derivatives from readily available starting materials.
Antihyperglycemic Activity of Novel Naphthalenyl 3H-1,2,3,5-Oxathiadiazole 2-Oxides
Ellingboe, John W.,Lombardo, Louis J.,Alessi, Thomas R.,Nguyen, Thomas T.,Guzzo, Frieda,et al.
, p. 2485 - 2493 (2007/10/02)
A series of naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides was prepared and tested for antihyperglycemic activity in the db/db mouse, a model for type 2 (non-insulin dependent) diabetes mellitus.Substitution at the 1-,5-, or 8-positions of the naphthalene ring with a halogen was found to be beneficial to antihyperglycemic activity. 4--3H-1,2,3,5-oxathiadiazole 2-oxide (45), one of the most potent compounds in this series, was selected for further pharmacological evaluation.
Composition and process for promoting the growth of crop plants
-
, (2008/06/13)
Compounds of the formula wherein Ar is (substituted) phenyl or naphthyl, X is oxygen, sulfur, SO or SO2, n is 1-3 and R is CN or C(NH2)NOR1, (wherein R1 is preferably hydrogen) are useful as safeners in crop protection.
