6-methyl-2-phenyl-7h-oxazolo [3,2-b] [1,2,4] triazine (1) undersent ting transformation on treatment with ammonia and primary amines to afford the corresponding imidazol [1,2-b][1,2,4] triazine (2). treatment of (1) with hydrazine hydrate gave the corresponding 3-aryl-4h-1,2,4- triazino [4,3-b][1,2,4] triazin-8 (1h)-one (3).

A new series of potent 8-hydroxyquinolines was designed based on the newly resolved X-ray crystal structure of EGLN-1. Both alkyl and aryl 8-hydroxyquinoline-7-carboxyamides were good HIF-1alpha prolyl hydroxylase (EGLN) inhibitors. In subsequent VEGF induction assays, these exhibited potent VEGF activity. In addition, this class of compounds did show the ability to stabilize HIF-1alpha.

Abstract An efficient protocol for the synthesis of 3‐ethynyl‐2‐aryl‐bicyclo[3.1.0]hexenes through a gold‐catalyzed enyne cyclization was established in this work. Depending on specific substitution pattern, unusual cationic rearrangements corresponding gold carbene were revealed, leading to either cyclohexadienes or 5,9‐methanobenzo[8]annulene derivatives, respectively.

Five new 2,9,9-trimethyl-6,7,8,9-tetrahydro-benzocyclohepten-5-ylidene-amine derivatives (16a-16e) were synthesized from α-dehydro-ar-himachalene (11) that was originally prepared from an isomeric mixture of α, β and γ himachalenes (10), the abundant sesquiterpenes of Cedrus deodara essential oil. In addition, different aryl himachalenes derivatives (9, 12, 14 and 15) were also formed from 11. ...

1,2,3-Triaminoguanidinium chloride was combined with benzaldehyde and hydratropic aldehyde to furnish the corresponding tris(imines), which were converted into 1,2,3-tris(benzylamino)guanidinium salts by catalytic hydrogenation in the former, and by borane reduction in the latter case. The resulting alkyl-substituted triaminoguanidinium salts underwent a threefold carbamoylation with aryl isocy...

A simple yet effective strategy for synthesis of 5-aryl-8-quinolinolate-based electroluminophores with tunable emission wavelengths is presented. Two different pathways for the attachment of electron-donating or electron-withdrawing aryl groups to the 5-position of the quinolinolate ligand via Suzuki coupling were developed. A successful tuning in the emission color was achieved: the emission w...

Experimental evidence is provided for p-methylbenzyl-D-galactonoamidine to function as a true transition state analog for the enzymatic hydrolysis of aryl-β-D-galactopyranosides by β-galactosidase (A. oryzae). The compound exhibits inhibition constants in the low nanomolar concentration range (12-56 nM) for a selection of substrates. Along these lines, a streamlined synthetic method based on ph...

In the title compound, C(12)H(10)BrN, the dihedral angle between the benzene rings is 52.5 (1)°, whereas the pitch angles, or the angles between the mean plane of each aryl group 'propeller blade' and the plane defined by the aryl bridging C-N-C angle, are 19.6 (2) and 36.2 (3)°. While the N-H group is not involved in hydrogen-bonding inter-actions, the structure exhibits a network of inter-mol...

8-Arylinosines have been scarcely studied for therapeutic purposes, probably due to difficulties in their synthesis. The recently described direct arylation reaction at position 8 of purine nucleosides has been employed to synthesize a series of 8-aryl and 8-pyridylinosines. These compounds have been studied for hydrolytic stability and subjected to biological evaluation. Three compounds have s...

In the cation of the title compound, C(5)H(8)N(3) (+)·I(-), the C-N(H(2)) bond distance [1.338 (8) Å] is at the lower end of the range for aryl amines. In the crystal structure, cations and anions are linked via N-H⋯I hydrogen bonds, forming centrosymmetric four-component clusters.