Novel acyl hydrazide derivatives of polyhydroquinoline as potent anti-diabetic and anti-glycating agents: Synthesis, in vitro α-amylase, α-glucosidase inhibition and anti-glycating activity with molecular docking insights.

In this study, eleven novel acyl hydrazides derivative of polyhydroquinoline were synthesized, characterized and screened for their in vitro anti-diabetic and anti-glycating activities. Seven compounds 2a, 2d, 2i, 2 h, 2j, 2f, and 2 g exhibited notable α-amylase inhibitory activity having IC50 values from 3.51 ± 2.13 to 11.92 ± 2.30 µM. Similarly, six compounds 2d, 2f, 2 h, 2i, 2j, and 2 g displayed potent α-glucosidase inhibitory activity compared to the standard acarbose. Moreover, eight derivatives 2d, 2 g, 2f, 2j, 2a, 2i, 2 g, and 2e showed excellent anti-glycating activity with IC50 values from 6.91 ± 2.66 to 15.80 ± 1.87 µM when compared them with the standard rutin (IC50 = 22.5 ± 0.90 µM). Molecular docking was carried out to predict the binding modes of all the compounds with α-amylase and α-glucosidase. The docking analysis revealed that most of the compounds established strong interactions with α-amylase and α-glucosidase. All compounds fitted well into the binding pockets of α-amylase and α-glucosidase. Among all compounds 2a and 2f were most potent based on docking score -8.2515 and -7.3949 against α-amylase and α-glucosidase respectively. These results hold promise for the development of novel candidates targeted at controlling postprandial glucose levels in individuals with diabetes.

Novel hydrogel poly (GG-co-acrylic acid) for the sorptive removal of the color Rhodamine-B from contaminated water.

Textile effluent's treatment is highly desired due to the presence of hazardous, water-soluble and non-biodegradable dyes that not only have harmful effect on the environment but on living beings as well. Treatment of these pollutants by sorption through biosorbents is considered to be a best method of choice due to greener nature of the processes. In this connection hydrogel sorbents might be an intriguing option due to its straightforward application, great efficacy, easy synthesis, rapid turnaround, and potential of recycling. Herein, novel hydrogel was prepared using Gellan Gum and acrylic acid (GG-co-AAc) which were then characterized by instrumental techniques like UV/visible and FTIR spectroscopy, SEM, EDX and XRD. The anionic hydrogel's adsorption capacity, swelling behavior, and sorption potential were determined using Rhodamine-B as potential environmental pollutant. The hydrogel exhibited an impressive adsorption capacity of 1250 mg/g. Swelling experiments were performed in Milli-Q distilled water at different pH levels, reaching maximum swelling of 3230% after 23 h as determined through Fickian diffusion. At pH 7, the anionic hydrogel's sorption potential was thoroughly studied in the subsequent experiments. The adsorption process was found to follow the Langmuir isotherm, indicating a monolayer adsorption mechanism supported by higher R2 values compared to the Freundlich isotherm. Thermodynamic analysis revealed the exothermic nature of the adsorption process, with a negative enthalpy value of -11371 KJmol-1 and negative entropy value of -26.39 Jmol-1K-1, suggesting a less ordered system. These findings provide valuable insights into the adsorption characteristics and potential applications of the synthesized anionic hydrogel.

Enhancing Dissolution Rate and Antibacterial Efficiency of Azithromycin through Drug-Drug Cocrystals with Paracetamol.

Cocrystallization is a promising approach to alter physicochemical properties of active pharmaceutical ingredients (hereafter abbreviated as APIs) bearing poor profile. Nowadays pharmaceutical industries are focused on preparing drug-drug cocrystals of APIs that are often prescribed in combination therapies by physicians. Physicians normally prescribe antibiotic with an analgesic/antipyretic drug to combat several ailments in a better and more efficient way. In this work, azithromycin (AZT) and paracetamol (PCM) cocrystals were prepared in 1:1 molar ratio using slow solvent evaporation method. The cocrystals were characterized by Fourier transform infrared (FTIR), Raman spectroscopy, powder X-ray diffraction (PXRD), differential scanning calorimeter (DSC), thermo gravimetric analysis (TGA) and high-performance liquid chromatography (HPLC). Vibrational spectroscopy and DSC confirmed that both APIs interact physically and showed chemical compatibility, while PXRD pattern of the starting material and products revealed that cocrystal have in a unique crystalline phase. The degree of hydration was confirmed by TGA analysis and result indicates monohydrate cocrystal formation. The HPLC analysis confirmed equimolar ratio of AZT:PCM in the cocrystal. The in vitro dissolution rate, saturation solubility, and antimicrobial activity were evaluated for AZT dihydrate and the resulting cocrystals. The cocrystals exhibited better dissolution rate, solubility and enhanced biological activities.

2-Benzyl-3-phenyl-1-(pyridin-2-yl)propan-1-one.

Mol-ecules of the title compound, C(21)H(19)NO, assume an approximate propellar shape, with the three aromatic rings being nearly perpendicularly aligned with respect to the plane formed by the C atoms that are connected to the methine C atom [dihedral angles: pyridyl 79.82 (4)°, phenyl 80.12 (3)° and phenyl 86.93 (3)°].

1-(Pyridin-2-yl)-2-[2-(trifluoro-meth-yl)benz-yl]-3-[2-(trifluoro-meth-yl)phen-yl]propan-1-one.

The title compound, C(23)H(17)F(6)NO, crystallizes with two mol-ecules in the asymmetric unit. The mol-ecules assume an approximate propellar shape, with the three aromatic rings being bent with respect to the plane formed by the C atoms that are connected to the methine C atom [dihedral angles: pyridyl 67.49 (3)°, phenyl 56.82 (4)° and phenyl 77.21 (6)° in one mol-ecule, and corresponding angles of 71.60 (6), 53.68 (4) and 77.53 (6)° in the second mol-ecule].