This study investigated the anticonvulsant activity of a new phthalazine tetrazole derivative, QUAN-0808 (6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine), in the mouse maximal electroshock (MES) seizure model. The neurotoxicity of QUAN-0808 was investigated using the rotarod neurotoxicity test in mice. QUAN-0808 exhibited higher activity (median effective dose, ED(50) = 6.8 mg/kg) and lower ne...

4'-Thio-2'-deoxycytidine was synthesized as a 5'- protected phosphoramidite compatible with solid phase DNA synthesis. When incorporated as the target cytosine (C*) in the GC*GC recognition sequence for the DNA methyltransferase M. HhaI, methyl transfer was strongly inhibited. In contrast, these same oligonucleotides were normal substrates for the cognate restriction endonuclease R. HhaI and it...

In the crystal structure of the title compound, C28H36I2S3, a terthio-phene monomer, the central thio-phene unit is arranged anti-coplanar to the two outer thio-phene rings. There are two crystallographically independent mol-ecules in the asymmetric unit, which show different conformations. In one mol-ecule, the dihedral angles between the inner and the two outer thiophene rings are 15.7 (3) an...

Primary and secondary kinetic and equilibrium isotope effects are calculated with density-functional methods for the in-line dianionic methanolysis of the native (unsubstituted) and thio-substituted cyclic phosphates. These reactions represent reverse reaction models for RNA transesterification under alkaline conditions. The effect of solvent is treated with explicit (single and double) water m...

In the title compound, C18H12F4N2S2, a bis-thio-phenyl Schiff base ligand with a perifluorinated aromatic core, the complete molecule is generated by crystallographic inversion symmetry. The thio-phene and tetra-fluorinated benzene rings are oriented at a dihedral angle of 77.38 (4)°. The crystal structure exhibits C-H⋯F hydrogen bonds, resulting in supra-molecular chains along the c-axis direc...

In the title compound, C11H7N3S, the thio-phene and pyridine rings are coplanar, forming a dihedral angle of 3.89 (7)°. The conformation about the C=N bond [1.2795 (18) Å] is E. In the crystal, translationally related mol-ecules along the a axis form weak π-π inter-actions [centroid-centroid distance = 3.8451 (8) Å] between the thio-phene rings.

In the title compound, [Cu(NCS)(C3H9PS)] n , the thio-cyanate ions bind the Cu(I) atoms covalently, forming infinite -Cu-SCN-Cu- chains parallel to the a axis. Each Cu(I) atom is also coordinated to a tri-methyl-phosphine sulfide group via a Cu-S bond. Two crystallographically independent chains propagate in opposite directions, and are held together in a ribbon arrangement by long bonds betwee...

Platelet P2Y12 is an important adenosine diphosphate (ADP) receptor that is involved in agonist-induced platelet aggregation and is a valuable target for the development of anti-platelet drugs. Here we characterise the effects of thio analogues of uridine triphosphate (UTP) on ADP-induced platelet aggregation. Using human platelet-rich plasma, we demonstrate that UTP inhibits P2Y12 but not P2Y₁...

The present study investigated the effect of thioperamide (THIO), an H3 histaminergic receptor antagonist, microinjected into the cerebellar vermis on emotional memory consolidation in male Swiss albino mice re-exposed to the elevated plus-maze (EPM). We implanted a guide cannula into the cerebellar vermis using stereotactic surgery. On the third day after surgery, we performed behavioral tests...