A series of novel dihydropyrazolo[3,4-d]pyrimidine derivatives bearing a phenothiazine nucleus were synthesized in excellent yields via a modified Biginelli multicomponent reaction. The newly synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR, Mass spectra and elemental analysis followed by antimycobacterial screening. Among all the screened compounds, compound 4g showed most pronounced activity against Mycobacterium tuberculosis (Mtb) with minimum inhibitory concentration (MIC) of 0.02μg/mL, making it more potent than first line antitubercular drug isoniazid.
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http://dx.doi.org/10.1016/j.bmcl.2014.02.012 | DOI Listing |
J Psychopharmacol
December 2024
Department of Psychiatry, Parnassia Groep BV, The Netherlands.
Background: Research on the pharmacogenetic influence of hepatic enzyme 2D6 () on metabolism of drugs for psychosis and associated outcome has been inconclusive. Some results suggest increased risk of adverse reactions in poor and intermediate metabolizers, while others find no relationship. However, retrospective designs may fail to account for the long-term pharmacological treatment of patients.
View Article and Find Full Text PDFSci Rep
May 2024
Department of Pharmacy, Mie University Hospital, 174-2, Edobashi, Tsu, Mie, 514-8507, Japan.
Sci Rep
May 2024
Department of Mathematics, Faculty of Science, Ramkhamhaeng University, Ramkhamhaeng Rd., Bangkok, 10240, Thailand.
This study employs a combination of mathematical derivation and optimization technique to investigate the adsorption of drug molecules on nanocarriers. Specifically, the chemotherapy drugs, fluorouracil, proflavine, and methylene blue, are non-covalently bonded with either a flat graphene sheet or a spherical fullerene. Mathematical expressions for the interaction energy between an atom and graphene, as well as between an atom and fullerene, are derived.
View Article and Find Full Text PDFJ Fluoresc
May 2024
Dyeing, Printing and Textile Auxiliaries Department, Textile Research and Technology Institute, National Research Centre, 33 EL Buhouth St., Dokki, Giza, 12622, Egypt.
Highly solid-state fluorescent dyes based on phenothiazine bearing sulfa-drug derivatives were successfully prepared and fully characterized by NMR, mass spectra, and elemental analysis. The prepared phenothiazine dyes bearing sulfadiazine and sulfathiazole 4-(((10-hexyl-10 H-phenothiazin-3-yl)methylene)amino)-N-(pyrimidin-2yl) benzenesulfonamide (PTZ-1) and 4-(((10-hexyl-10 H-phenothiazin-3-yl) methylene) amino)-N-(thiazol-2-yl)benzenesulfonamide (PTZ-2), showed strong emission in polycrystalline form, and significant emission in solution was observed. The quantum yield of the prepared dyes varied and decreased by increasing the solvent polarity, with the maximum recorded value being 0.
View Article and Find Full Text PDFJ Vasc Interv Radiol
July 2024
RenovoRx, Los Altos, California. Electronic address:
Purpose: Treatment of hypovascular tumors, such as pancreatic adenocarcinoma, is challenging owing to inefficient drug delivery. This report examines the potential mechanism of localized drug delivery via transarterial microperfusion (TAMP) using a proprietary adjustable double-balloon occlusion catheter in a porcine model.
Materials And Methods: Adult Yorkshire swine (N = 21) were used in the Institutional Animal Care & Use Committee-approved protocols.
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