The properties relevant to pharmacokinetics and pharmacodynamics of four series of synthesized s-triazine derivatives have been studied by Quantitative structure-retention relationship (QSRR) approach. The chromatographic behavior of these compounds was investigated by using reversed-phase high performance thin-layer chromatography (RP-HPTLC). Chromatographic retention (RM0) was correlated with...

High-throughput screening identified the imidazo[1,2-a]pyridine and bisanilinopyrimidine series as inhibitors of the cyclin-dependent kinase CDK4. Comparison of their experimentally-determined binding modes and emerging structure-activity trends led to the development of potent and selective imidazo[1,2-a]pyridine inhibitors for CDK4 and in particular CDK2.

In the title methanol-solvated salt, C14H19Cl3N5O2 (+)·Cl(-)·CH3OH, the triazine mol-ecule is protonated at one of the triazine N atoms. In the crystal, the triazine cations are linked through a pair of N-H⋯N hydrogen bonds, with graph-set R 2 (2)(8), forming an inversion dimer. The protonated N atom and the 2- and 4-amino groups of the triazine cation inter-act with the chloride anion through ...

In the title 1,2,4-triazine derivative, C(17)H(19)N(3)O(3), the heterocyclic ring is planar (r.m.s. deviation = 0.040 Å) and effectively coplanar with the adjacent phenyl ring [dihedral angle = 4.5 (2)°] but almost perpendicular to the (cyclo-hex-3-en-1-ylmeth-oxy)methyl residue [N-N-C-O torsion angle = 71.6 (5)°], so that the mol-ecule has an 'L' shape. Supra-molecular chains along [001] are f...

A series of 1,2,4-triazine derivatives Va (1-24) and Vb (1-24) were synthesized and evaluated for their anti-anxiety and anti-inflammatory activities. The structures of the synthesized compounds were confirmed on the basis of their spectral data. Many of the triazine compounds were found to possess good activity. Especially, compounds bearing the sulfur atom showed better activity than those be...

Various 2-amino-3-acyl-6-[(E)-1-phenyl-2-N-methylcarbamoylvinyl]-imidazo[1 ,2-a]pyridines, structurally related to Enviroxime were prepared to determine the effect of acyl groups on the anti-rhinoviral activity. A short and efficient means for the construction of the imidazo nucleus as well as biological evaluation of the final compounds are disclosed.

A new dimension: The doping of amorphous poly(triazine imide) (PTI) through ionothermal copolymerization of dicyandiamide with 4-amino-2,6-dihydroxypyrimidine (4AP) results in triazine-based carbon nitrides with increased photoactivity for water splitting compared to crystalline poly(triazine imide) (PTI/Li(+)Cl(-), see picture) and melon-type carbon nitrides. This family of carbon nitride semi...

Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole ...

A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure-activity relationships of these inhi...

Copper bromide catalyzed aerobic oxidative coupling of 2-aminopyridines with cinnamaldehydes directly led to the formation of 3-formyl-2-phenyl-imidazo[1,2-a]pyridines. The quantum chemical calculations were performed to trace the reaction mechanism and get insights into the possible reaction pathway. 2-Aminopyridines on coupling with cinnamaldehyde generate (E)-3-phenyl-3-(pyridin-2-ylamino)ac...