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Z. Naturforsch. 58b, 106 – 110 (2003); received September 18, 2002 Benzyloxyureas (4) have been prepared by reactions of diethyl 3-benzyloxyamino-propyl-phosphonate (3) with isocyanates, potassium cyanate or 1,1’-carbonyldiimidazole / methylamine. Conversion of phosphonic esters 4 into phosphonic acids 6 by means of bromotrimethylsilane and catalytic(More)
3-Hydroxy-N'-arylidenepropanehydrazonamides represent a new class of antiplasmodial compounds. The two most active phenanthrene-based derivatives showed potent in vitro antiplasmodial activity against the 3D7 (sensitive) and Dd2 (multidrug-resistant) strains of Plasmodium falciparum with nanomolar IC50 values in the range of 8-28 nM. Further studies(More)
This research was carried out to study the pharmacological activity of a newly synthesized series of 2-alkoxy-[1,2,4]triazolo[1,5-a]quinazolin-5-ones as adenosine receptor antagonists. These compounds have been tested in radioligand binding assays on cloned Chinese hamster ovary (CHO) cells transfected with A(1), A(2A), A(2B) and A(3) receptors. In(More)
Two series of pyrazolo[4,3-d]pyrimidin-7-ones and pyrido[2,3-d]pyrimidin-4-ones were designed, synthesised, and evaluated for their antibacterial activities and CDKs inhibitory activities. The pyridazine derivative: 6-phenyl-5-phenylhydrazono-2,3,4,5-tetrahydropyridazine-3,4-dione (3a) revealed activity against Staphylococcus aureus as Gram-positive(More)
A series of 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives has been prepared and subsequently evaluated with regards to the inhibition of 5-LOX/COX. Structure optimization furnished derivatives with promising in vitro activity as dual 5-LOX/COX inhibitors with submicromolar IC(50) values for inhibition of 5-LOX and COX-1, respectively.
In the cation of the title salt, C(11)H(12)IN(4) (+)·Cl(-), the two aromatic rings are oriented to each other at 9.3 (2)°. In the crystal, the two independent Cl(-) anions lie on twofold rotation axes. N-H⋯Cl hydrogen bonds between the cations and anions generate a supra-molecular layer parallel to (010).
The anthranilic scaffold plays an important role as a pharmacophore and toxophore in medicinal and agricultural chemistry and contributes to a variety of biological activities [1 – 9]. Although ring-closure reactions of N-unsubstituted anthranilic acid derivates have been extensively elaborated, investigations towards the corresponding chemistry of(More)
A series of previously unreported α-hydroxy hydrazonates were synthesized and tested for their antimalarial properties. Structure optimization of the antiplasmodially active α-hydroxy hydrazonate III furnished derivatives with strong in-vitro antimalarial activity against 3D7 strains of Plasmodium falciparum with IC(50) values lower than 2.0 µM.