Closed 2-Form of 2D Black Holes from Geometric Prequantization Method

In this paper, we consider effective Hamiltonian of 2D dilatonic black hole adding Axion field and calculate closed 2-form by using geometric prequantization method. It yields to the Schrödinger equation which may be solved to obtain wave function. We obtained a condition on the cosmological constant to obtain appropriate Hamilton equation of motions.     

BSA Interaction,Molecular Docking,and Antibacterial Activity of Zinc(II) Complexes Containing the Sterically Demanding Biomimetic N3S2 Ligand: The Effect of Structure Flexibility

Two zinc(II) complexes, DBZ and DBZH₄, that have (ZnN₃S₂) cores and differ in the bridging mode of the ligating backbone, effectively bind to BSA. The binding affinity varies as DBZ > DBZH₄ and depends on the ligand structure. At low concentrations, both complexes exhibit dynamic quenching, whereas at higher concentrations they exhibit mixed (static and dynamic) quenching. The energy transfer mechanism from the BSA singlet excited state to DBZ and DBZH₄, is highly likely according to steady-state fluorescence and time-correlated singlet photon counting. Molecular docking was used to support the mode of interaction of the complexes with BSA and showed that DBZ had more energy for binding. Furthermore, antibacterial testing revealed that both complexes were active but to a lesser extent than chloramphenicol. In comparison to DBZH₄, DBZ has higher antibacterial activity, which is consistent with the binding constants, molecular docking, and particle size of adducts. These findings may have an impact on biomedicine.     

Synthesis of 3-cyano-2-pyridone derivative and its utility in the synthesis of some heterocyclic compounds with expecting antimicrobial activity

New 2-pyridone derivatives bearing p-methoxyphenyl and p-bromophenyl substituents at C-4 and C-6 were prepared smoothly by the one-pot reaction in high yield, and in a comparatively short time, it reacted with phosphorous oxychloride to produce the corresponding chloro compound. The latter was reacted with several nitrogen nucleophiles such as sodium azide, hydrazine, acetohydrazide, and benzohydrazide to give tetrazolo, hydrazino, and triazolo derivatives, respectively. The reaction of hydrazino derivative with cyclopentanone, furan-2-carbaldehyde afforded the corresponding hydrazone derivatives. Cyclocondensation of the latter compounds with thioglycolic acid afforded the nicotinamide derivatives. 2-Pyridone reacted with ethyl chloroacetate to afford chloroacetate and ethyl acetate derivatives. Ethyl acetate-derivative reacted with hydrazine hydrate and gave the acetohydrazide derivative, it was condensed with p-anisaldehyde and gave the 4-methoxybenzylidene acetohydrazide derivative. Also, 2-pyridone reacted with chloroacetic acid and or benzoyl chloride, afforded the benzoate derivative and 2-((6-(4-bromophenyl)-3-cyano-4-(4-methoxyphenyl) pyridin-2-yl) oxy) acetic acid, respectively. Structures of the products were confirmed using spectroscopic data and elemental analyses. Antibacterial activity of the synthesized compounds was evaluated against Escherichia coli and Staphylococcus aureus.     

Corrosion Inhibitors: Quantitative Structure–Activity Relationships

Quantitative structure–activity relationships (QSAR) between corrosion inhibition efficiency and molecular structure may help promote the discovery of new, more efficient corrosion inhibitors. In this work various methods used in the QSAR studies of corrosion inhibitors are reviewed and discussed briefly.     

Efficient synthesis of CN2097 using in situ activation of sulfhydryl group

CN2097 (R₇Cs-sCYK[KTE(β-Ala)]V) is a rationally designed peptidomimetic that shows effectiveness in preclinical models for the treatment of neurological disorders, such as Angelman syndrome, traumatic brain injury (TBI), and stroke. Because of its potential therapeutic activity for the treatment of human CNS disorders, there was an urgent need to develop an efficient strategy for large-scale synthesis of CN2097. The synthesis of CN2097 was accomplished using Fmoc/tBu solid phase chemistry in multiple steps. Two different peptide fragments (activated polyarginine peptide Npys-sCR₇ and CYK[KTE(β-Ala)]V) were synthesized, followed by solution phase coupling in water. Activation of the polyarginine (CR₇) was achieved in situ during cleavage of protected peptide (C(Trt)R(Pbf)₇) from the Rink amide resin using 5 equiv. of 2,2-dithopyridine in TFA:TIS:H₂O (95:2.5:2.5, v/v/v) for 4 h. The disulfide coupling was efficient which provided a 60% yield.