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A series of sildenafil analogues and aniline substituted pyrazolo[4,3-e][1,2,4]triazine sulfonamides were prepared and evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors and for their anticancer activity against two human breast cancer cell lines (MCF-7, MDA-MB-231). The new compounds were ineffective as CA I inhibitors, poorly inhibited CA II, but(More)
In the search for new biologically active chemotypes, several sildenafil analogs were prepared and characterized. The presence of the pyrazolo[4,3-e][1,2,4]triazine core is thought to be of interest for the enzyme inhibitory activity of these compounds. The designed derivatives incorporating the sildenafil scaffold were assayed as carbonic anhydrase(More)
In the title compound, C(7)H(9)N(5)O(2)S, the pyrazolo-[4,3-e][1,2,4]triazine fused-ring system is essentially planar [maximum deviation = 0.0420 (3) Å]. In the crystal, mol-ecules related by twofold axes are linked into a mol-ecular net via inter-molecular C-H⋯O and C-H⋯N hydrogen bonds. π-π inter-actions are observed between the triazine and pyrazole(More)
The title compound, C21H16N4, obtained under standard Suzuki cross-coupling conditions, is a model compound in the synthesis and biological activity evaluation of new aza-analogues of sildenafil containing a pyrazolo-[4,3-e][1,2,4]triazine system. An N-H⋯N intra-molecular hydrogen bond involving the amino-benzene system and the 1,2,4-triazine moiety helps(More)
A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their tyrosinase and urease inhibitory activity. Evaluation of prepared derivatives demonstrated that compounds (8b) and (8j) are most potent mushroom tyrosinase inhibitors whereas all of the(More)
Synthesis of several pryrazolo[4,3-e][1,2,4]-triazines is described. The absorption spectrum of some 5-substituted derivatives was found to extend to the visible region. These compounds were found to inhibit some enzymes of purine metabolism, like xanthine oxidase or bacterial purine-nucleoside phosphorylase with Ki values in the 10(-3) -10(-5) M range.
The mol-ecule of the title compound, C(12)H(14)N(8)S(2), has an N-N gauche conformation. The triazine rings are nearly coplanar with respect to the imide bonds [C-C-C-N torsion angles = -15.3 (3) and -15.8 (3)°] and they are twisted by 77.88 (7)°. The overall conformation of the mol-ecule is stabilized by intra-molecular C-H⋯N hydrogen bonding. The(More)
A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their relaxant effects in the rat aorta. Evaluation of prepared derivatives demonstrated that compound (8a) is probably a non-selective phosphodiesterase (PDE) inhibitor, as it induced aortic(More)
The title compound, C(10)H(10)N(2)O(2), was synthesized by the reaction of the oxime of 2-acetyl-pyridine and 3-bromo-propanoyl chloride in the presence of triethyl-amine. The mol-ecule adopts a nearly planar chain-extended conformation with the oxime group in a trans and the acryloyl group in an s-cis conformation. This conformation is stabilized by an(More)
A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine has been synthesized and characterized. Their anticancer activity was tested in vitro against multiple human cancer cell lines and were found to have dose-dependent antiproliferative effects. Furthermore, some of the new compounds inhibited the Abl protein kinase with low micromolar(More)