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Compound L-36, a new derivative of 6H-1,3,4-thiadiazine, was studied in in vitro and in vivo experiments. This compound exhibits high antiplatelet and antithrombogenic activity. In in vitro experiments, compound L-36 by its antiplatelet activity (by IC 50 ) was superior to acetylsalicylic acid by 9.4 times. In in vivo experiments, compound L-36 by its ED 50 value was close to the comparison drug. On the model of pulmonary artery thrombosis, compound L-36 ensured better survival of experimental animals than acetylsalicylic acid. Morphological studies showed that compound L-36 effectively attenuated the thrombosis processes in the pulmonary tissue induced by intravenous injection of a thrombogenic mixture (epinephrine and collagen)., (© 2024. Springer Science+Business Media, LLC, part of Springer Nature.)

Extensive application of pesticides has caused a lot of environmental pollution and health problems, prompting the development of highly efficient and lowly toxic pesticide formulations. Here, buprofezin (BPF)-loaded poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) (P(HB-HH)) microspheres were prepared by O/W emulsion/solvent evaporation method. Under optimal conditions (P(HB-HH) 7.07% (w/v) and PVA 1.84% (w/v)), the spherical and monodispersed microspheres were obtained. The average particle size, pesticide loading (PL), and encapsulation efficiency (EE) of the optimized microspheres were 1.2 μm, 15.68%, and 78%, respectively. Release of 80% BPF from the microspheres in pH 5 (192 h) was faster than that in pH 7 (228 h) and 8 (204 h). Moreover, kinetic analysis indicated that BPF release behaved in a non-Fickian diffusion manner (0.43 < n < 0.85) and the release mechanism was the combined effects of pesticide diffusion and hydrolysis of polymer. The bioassay and toxicity results showed that encapsulation of BPF could exhibit high efficacy on the target organism and low toxicity to the non-target organism. Therefore, these results demonstrated that BPF-loaded P(HB-HH) microspheres with good stability were prepared successfully, and they could be further explored for constructing other highly efficient and lowly toxic pesticide formulations.

The enzyme adenosine kinase (AK) plays a key role in the regulation of intracellular and extracellular concentration of adenosine (Ado), which exhibits potent hormonal activity in cardiovascular, nervous and immune systems. In view of the pharmacological effects of Ado, there is much interest in identifying inhibitors of AK, which can augment its tissue-protective effects. In this study, we have screened 1040 compounds from a chemical library of putative kinase inhibitors for their effect on purified human recombinant AK. These studies have identified 8 novel, non-nucleoside AK inhibitors. Four of these compounds (viz. 2-tert-butyl-4H-benzo[1,2,4]thiadiazine-3-thione (2759-0749); N-(5,6-diphenyl-furo[2,3-d]pyrimidin-4-yl)-propionamide (3998-0118); 3-[5,6-Bis-(4-methoxy-phenyl)-furo[2,3-d]pyrimidin-4-ylamino]-propan-1-ol (4072-2732); and 2-[2-(3,4-dihydroxy-phenyl)-5-phenyl-1H-imidazol-4-yl]-fluoren-9-one (8008-6198)), which inhibited human AK in a concentration-dependent manner in a low micromolar range (IC(50) = 0.38 approximately 1.98 microM) were further studied. Kinetic and structural studies on these compounds provide evidence that inhibition of AK by these compounds was competitive with respect to Ado and non-competitive for ATP. All of these compounds also inhibited uptake of Ado and its metabolism in cultured mammalian cells at comparable concentrations indicating their efficient cellular penetrability. These AK inhibitors, whose chemical structures differ significantly from all previously known inhibitors, provide useful lead compounds for identification of more potent but less toxic AK inhibitors that may prove useful for therapeutic purposes.

A chelating resin coupling Amberlite XAD-2 functionalized with dithizone is synthesized and characterized. Dissolved cadmium is field-preconcentrated using a minicolumn packed with the synthesized resin and determined by flame atomic absorption spectrometry. Five experimental variables are evaluated. The enrichment factor of 416 is obtained for 50 mL of sampling volume, and the detection limit (3 sigma) of the procedure is 6.7 ng L(-1). The precision (RSD) for 11 independent determinations is 1.97%. This method has been successfully applied to the determination of cadmium in natural seawater samples.

Hydrogen bond complex stability between adenine (A) and hydrogen bond equivalents of uracil: 2-pyridone derivatives (U(X2O)X) and 3-oxo-1,2,6-thiadiazine-1,1-dioxide derivatives (U(SO2)X) was studied, and as the result, the hydrogen bond energy of U(X2O)X-A and a complex of UX(SO2)X-A, was about 1.5 kcal/mol more stable than that of the corresponding adenine-uracil derivatives complex, respectively. The energy difference between the imide tautomer and enol tautomer was smaller than those of uracil derivatives. U(SO2)F can form a stable complex with A, and its imide tautomer is stable.