Search

In an endeavor to invent new antimalarial and antimicrobial agents, a series of coumarin bound 1,4-disubstituted 1,2,3-triazoles was synthesized through Cu(I)-promoted click reaction between coumarin bound terminal alkynes, that is, 4/7-(prop-2-yn-1-yloxy)-2H-chromen-2-one and 2-azido-N-arylpropanamides. The synthesized 1,2,3-triazoles were characterized by FTIR,1H NMR,13C NMR, and HRMS techniques and were assessed for in vitro antimalarial activity against Plasmodium falciparum as well as in vitro antimicrobial activity against four bacterial strains (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Klebsiella pneumoniae) and two fungal strains (Candida albicans, Aspergillus niger). Compound 7o [(N-(4-fluorophenyl)-2-(4-(((2-oxo-2H-chromen-7-yl)oxy)methyl)-1H-1,2,3-triazol-1-yl)propanamide)] displayed better activity against P. falciparum while compound 7y [(N-(3-nitrophenyl)-2-(4-(((2-oxo-2H-chromen-7-yl)oxy)methyl)-1H-1,2,3-triazol-1-yl)propanamide)] displayed excellent activity against all the tested bacterial and fungal strains, amongst the synthesized triazoles. Also, the molecular docking studies of the most potent compounds against DNA gyrase (S. aureus) were also performed to have an insight on binding interactions. [ABSTRACT FROM AUTHOR]

A series of quinoline-thiazole appended 1,4-disubstituted 1,2,3-triazole were synthesized by performing Cu(I) catalyzed 1,3-dipolar cycloaddition reaction ("Click" reaction) and fully characterized by various spectral techniques like FTIR, NMR and HRMS. These compounds were evaluated for in vitro antimalarial activity against plasmodium falciparum. All the compounds (7a–7y) exhibited moderate to good activity in comparison to standard drug Quinine. Compound 7r (IC50 0.19 µg/mL) displayed appreciable activity comparable to Quinine (IC50 0.268 µg/mL). Further antimicrobial screening of the synthesized substituted triazoles were also carried out against two gram (+) bacteria (Staphylococcus aureus, Bacillus subtilis), two gram (–) bacteria (Escherichia coli, Klebsiella pneumonia) and two fungi (Candida albicans, Aspergillus niger). Results revealed that compound 7r reflected promising antimicrobial activity among the synthesized library of molecules. Molecular docking studies of broadly active antimalarial disubstituted triazoles 7m and 7r were explored in the active site of enzyme dihydroorotate dehydrogenase (DHODH) to have the probable mode of action. [ABSTRACT FROM AUTHOR]

The aim of this study was to conduct a technical and clinical evaluation of a Silicon Photomultiplier (SiPM) integrated digital Positron Emission Tomography – Computed Tomography (PETCT) Scanner using National Electrical Manufacturers Association (NEMA) NU 2- 2018 standards. System sensitivity was measured by using a NEMA sensitivity phantom. Scatter fraction, count-rate performance, accuracy of count loss, and timing resolution were all computed. Clinical images were acquired and image quality was assessed and compared with published studies. At 1 cm, tangential, radial, and axial spatial resolutions were 3.02 mm, 3.02 mm, and 2.73 mm at full width half maximum (FWHM), respectively. Sensitivity at centre and 10 cm was 10.359 cps/kBq and 9.741 cps/kBq, respectively. The timing resolution was measured at 372 ps. The digital PETCT exhibits a high-spatial resolution and a superior timing resolution, which advances the diagnostic ability to detect small lesions and boosts the diagnostic confidence. Increases clinical relevance by improving the ability to detect and differentiate tiny or low-contrast lesions without compromising radiopharmaceutical dose or overall scan time. [ABSTRACT FROM AUTHOR]