RESUMO
The respiratory infection tuberculosis is caused by the bacteria Mycobacterium tuberculosis and its unrelenting spread caused millions of deaths around the world. Hence, it is needed to explore potential and less toxic anti-tubercular drugs. In the present work, we report the synthesis and antitubercular activity of four different (hydrazones 7-12, O-ethynyl oximes 19-24, triazoles 25-30, and isoxazoles 31-36) hybrids. Among these hybrids 9, 10, 33, and 34, displayed high antitubercular activity at 3.12 g/mL with >90% of inhibitions. The hybrids also showed good docking energies between -6.8 and -7.8 kcal/mol. Further, most active molecules were assayed for their DNA gyrase reduction ability towards M. tuberculosis and E.coli DNA gyrase by the DNA supercoiling and ATPase gyrase assay methods. All four hybrids showed good IC50 values comparable to that of the reference drug. In addition, the targets were also predicted as a potential binder for papain-like protease (SARS CoV-2 PLpro) by molecular docking and a good interaction result was observed. Besides, all targets were predicted for their absorption, distribution, metabolism, and excretion - toxicity (ADMET) profile and found a significant amount of ADMET and bioavailability.
RESUMO
The present study describes the synthesis of two new series of 3-hydroxy-N-(4-oxo-2-phenyl-1,3-thiazinan-3-yl)-8-(trifluoromethyl)quinoline-2-carboxamide derivatives (4a-j) and 3-((7-chloroquinolin-4-ylamino)methyl)-2-phenyl-1,3-thiazinan-4-one derivatives (5a-7j). All the compounds were synthesized in moderate to good yield by one-pot three component cyclo-condensation reaction. The newly synthesized compounds were characterized by FT-IR, 1H, 13C NMR and elemental analysis. The compounds were screened for their in vitro antibacterial activity against a panel of pathogenic bacterial strains, antitubercular activity against Mycobacterium tuberculosis H37Rv and also for their in vitro antimalarial activity against Plasmodium falciparum. Among the synthesized compounds two of them (4f and 5f) showed excellent antibacterial activity against C. tetani at 15.6µg/mL. Some of them exhibited excellent antitubercular (4f &5f) and good antimalarial (4f, 5f &6f) activity compared with the first line drugs.
Assuntos
Antibacterianos/síntese química , Antimaláricos/síntese química , Antituberculosos/síntese química , Quinolinas/química , Tiazinas/química , Antibacterianos/química , Antibacterianos/farmacologia , Antimaláricos/química , Antimaláricos/farmacologia , Antituberculosos/química , Antituberculosos/farmacologia , Clostridium tetani/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Plasmodium falciparum/efeitos dos fármacos , Quinolinas/síntese química , Espectroscopia de Infravermelho com Transformada de Fourier , Relação Estrutura-AtividadeRESUMO
In this work, silverbismuth oxide encapsulated 1,3,5-triazine-bis(4-methylbenzenesulfonyl)-hydrazone functionalized chitosan (SBO/FCS) nanocomposite was synthesized by a simple hydrothermal method. The amine (-NH2) group was functionalized by the addition of cyanuric acid chloride followed by 4-methylbenzenesulfonol hydrazide. The SBO/FCS has been characterized by FT-IR, X-ray diffraction, XPS, HR-SEM, HR-TEM, AFM, and thermogravimetry (TGA). Under the optimum conditions, the SBO/FCS sensor showed brilliant electrochemical accomplishment for the sensing of glucose and H2O2 by a limit of detection (LOD) of 0.057 µM and 0.006 µM. It also showed linearity for glucose 0.008-4.848 mM and for H2O2 of 0.01-6.848 mM. Similarly, the sensor exhibited a low sensitivity to glucose (32 µA mM-1 cm-2) and a good sensitivity to H2O2 (295 µA mM-1 cm-2). In addition, that the prepared electrode could be used to sense the glucose and H2O2 levels in real samples such as blood serum and HeLa cell lines. The screen printed electrode (SPE) immunosensor could sense the E. coli O157:H7 concurrently and quantitatively with a linear range of 1.0 × 101-1.0 × 109 CFU mL-1 and a LOD of 4 CFU mL-1. Likewise, the immunosensor efficiently detect spiked E. coli O157:H7 in milk, chicken, and pork samples, with recoveries ranging from 89.70 to 104.72 %, demonstrating that the immunosensor was accurate and reliable.
Assuntos
Técnicas Biossensoriais , Bismuto , Quitosana , Escherichia coli O157 , Nanocompostos , Humanos , Peróxido de Hidrogênio/química , Prata , Glucose , Técnicas Biossensoriais/métodos , Hidrazonas , Espectroscopia de Infravermelho com Transformada de Fourier , Células HeLa , Imunoensaio/métodos , Nanocompostos/químicaRESUMO
In this work, pure ZnZrO2 and chitosan supported (ZnZrO2/CS) nanocomposite have been synthesized at low coast by hydrothermal method. FT-IR, Micro Raman, PXRD, HR-SEM-EDAX, HR-TEM, AFM, BET and XPS were used to analyze the structural and morphological properties of the fabricated nanocomposites. The fabricated ZnZrO2 and ZnZrO2/CS nanocomposites were measured for their electrocatalytic activity towards glucose and hydrogen peroxide determinations. The ZnZrO2/CS sensor exhibited wide detection range (5 µM to 5.85 mM), high sensitivity (6.78 µA mM-1 cm-2), LOD (2.31 µM), and long-term stability for glucose detection in alkaline solution. Also, as a multifunctional electrochemical sensor, ZnZrO2/CS sensor exhibits excellent sensing ability towards hydrogen peroxide, with a wide dynamic range (20 µM to 6.85 mM), a high sensitivity (2.22 µA mM-1 cm-2), and a LOD (2.08 µM) (S/N = 3). The electrochemical measurement shows that the ZnZrO2/CS sensor has excellent catalytic activity and a much LOD than ZnZrO2. The modified electrode showed excellent anti interference nature. Furthermore, this ZnZrO2/CS electrode was used to detection of glucose and H2O2 in human blood serum and HeLa cells respectively.
Assuntos
Quitosana , Nanocompostos , Humanos , Peróxido de Hidrogênio , Quitosana/química , Glucose , Células HeLa , Espectroscopia de Infravermelho com Transformada de Fourier , Nanocompostos/química , Eletrodos , Técnicas Eletroquímicas/métodosRESUMO
In this study, silver-functionalized bismuth oxide (AgBi2O3) nanoparticles (SBO NPs) were successfully synthesized by a highly efficient hydrothermal method. The as-synthesized SBO nanoparticles were characterized using FT-IR, P-XRD, XPS, HR-SEM, and HR-TEM analytical methods. It was found that the NPs were in spherical shape and hexagonal crystal phase. The newly prepared SBO electrode was further utilized for the detection of glucose, NO2- and H2O2 by cyclic voltammetry (CV) and amperometric methods. The electrodes exhibited high sensitivity (2.153 µA mM-1 cm-2 for glucose, 22 µA mM-1 cm-2 for NO2- and 1.72 µA mM-1 cm-2 for H2O2), low LOD (0.87 µM for glucose, 2.8 µM for NO2- and 1.15 µM for H2O2) and quick response time (3 s for glucose, 2 s for both NO2- and H2O2 respectively). The sensor exhibited outstanding selectivity despite the presence of various interferences. The developed sensor exhibited good repeatability, reproducibility, and stability. In addition, the sensor was used to measure glucose, H2O2 in human serum, and NO2- in milk and river water samples, demonstrating its potential for use in the real sample.
RESUMO
In the title compound, C(22)H(23)N(3)O(2)S(2), the five-membered ring is planar and the C(5)S ring adopts a chair conformation. The crystal packing is stabilized by inter-molecular N-Hâ¯O and C-Hâ¯O inter-actions, generating a chain and a centrosymmetric dimer, respectively.
RESUMO
A series of 2,6-diaryltetrahydropyran-4-one thiosemicarbazones (11-27) were synthesized and characterized for evaluation of potential antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi, Bacillus subtilis and Klebsiella pneumonia and antifungal activity against Cryptococcus neoformans, Candida albicans, Rhizopus sp., Aspergillus niger and Aspergillus flavus were evaluated. Compounds 21 and 22 showed maximum inhibition potency at low concentration (6.25 µg/ml) against P. aeruginosa. For antifungal activity, 20 and 21 were effective against C. neoformans and 22-24 against C. albicans at minimum concentration. Further, the results of QSAR studies of these synthesized compounds indicated the importance of weakly polar component of surface area, hydrophobicity and ionization potential parameters in defining their antimicrobial activity.