Three series of novel and new fused heterocyclic systems, viz. triazolo[4,3-a]-quinazolin-7-ones (4), [1,2,4,5]-tetrazino[4,3-a]-quinazolin-8-ones (6) and indolo[2,3-c][1,2,4]-triazino[4,3-a]-quinazolin-8-ones (8) have been synthesized from the key intermediate 3-(substituted-phenyl)-2-hydrazino-quinazolin-4-ones (3). Thus, condensation of (3) with appropriate aromatic acids in the presence of DCC in dichloromethane afforded the fused system (4), while reaction of (3) with isatin in methanol gave the corresponding Schiff base (7) which on cyclodehydration furnished another fused heterocyclic system (8). The intermediate (3) on refluxing with substituted-phenylisothiocyanate gave the substituted-thiosemicarbazide (5), which on oxidative cyclization with bromine in CCl(4) furnished the novel fused system (6). The structures of intermediate and final compounds have been determined by means of IR, (1)H NMR, (13)C NMR, UV and elemental analysis. All the synthesized compounds have been screened for their antibacterial activity against gram-negative bacteria, Escherichia coli, Pseudomonas aeruginosa and gram-positive bacteria, Streptococcus pneumoniae, Bacillus subtilis, as well as demonstrated significant antifungal activity against fungi viz. Candida albicans, Aspergillus fumigatus, Aspergillus flavus, and Aspergillus niger.
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http://dx.doi.org/10.1016/j.ejmech.2008.05.033 | DOI Listing |
Eur J Med Chem
January 2025
Laboratory of Medicinal Chemical Biology, Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Suzhou Medical College, Soochow University, 199 Ren'ai Road, Suzhou, 215123, PR China. Electronic address:
Pleurotin (1) is a benzoquinone meroterpenoid known for its wide-spectrum antitumor and antibiotic activities, notably acting as natural inhibitors of the thioredoxin reductase (TrxR). Pleurotin (1) has been chemically synthesized, but only in milligram quantities through at least 13 longest linear steps with 0.8 % overall yield due to its complex structure such as fused hexacyclic core with 8 contiguous stereocenters.
View Article and Find Full Text PDFSensors (Basel)
December 2024
Key Laboratory of Opto-Electronic Information Processing, Chinese Academy of Sciences, Shenyang 110016, China.
Cross-view geo-localization (CVGL) aims to determine the capture location of street-view images by matching them with corresponding 2D maps, such as satellite imagery. While recent bird's eye view (BEV)-based methods have advanced this task by addressing viewpoint and appearance differences, the existing approaches typically rely solely on either OpenStreetMap (OSM) data or satellite imagery, limiting localization robustness due to single-modality constraints. This paper presents a novel CVGL method that fuses OSM data with satellite imagery, leveraging their complementary strengths to enhance localization robustness.
View Article and Find Full Text PDFPolymers (Basel)
January 2025
Research Laboratory of Asymmetric Synthesis and Molecular Engineering of Materials for Organic Electronic (LR18ES19), Department of Physics, Faculty of Sciences of Monastir, University of Monastir, Avenue of Environment, Monastir 5019, Tunisia.
This paper explores a novel group of D-π-A configurations that has been specifically created for organic solar cell applications. In these material compounds, the phenothiazine, the furan, and two derivatives of the thienyl-fused IC group act as the donor, the π-conjugated spacer, and the end-group acceptors, respectively. We assess the impact of substituents by introducing bromine atoms at two potential substitution sites on each end-group acceptor (EG1 and EG2).
View Article and Find Full Text PDFJ Immunother Cancer
December 2024
Department of Pathology and Laboratory Medicine, University of California Los Angeles, Los Angeles, California, USA
Background: Granzyme B (GrB) is a key effector molecule, delivered by cytotoxic T lymphocytes and natural killer cells during immune surveillance to induce cell death. Fusion proteins and immunoconjugates represent an innovative therapeutic approach to specifically deliver a deadly payload to target cells. Epithelial membrane protein-2 (EMP2) is highly expressed in invasive breast cancer (BC), including triple-negative BC (TNBC), and represents an attractive therapeutic target.
View Article and Find Full Text PDFJ Neural Eng
January 2025
Department of Pediatrics, Oregon Health & Science University, 3181 SW Sam Jackson Park Rd, Portland, Oregon, 97239-3098, UNITED STATES.
Objective: The RSVP Keyboard is a non-implantable, event-related potential-based brain-computer interface (BCI) system designed to support communication access for people with severe speech and physical impairments. Here we introduce Inquiry Preview, a new RSVP Keyboard interface incorporating switch input for users with some voluntary motor function, and describe its effects on typing performance and other outcomes.
Approach: Four individuals with disabilities participated in the collaborative design of possible switch input applications for the RSVP Keyboard, leading to the development of Inquiry Preview and a method of fusing switch input with language model and electroencephalography (EEG) evidence for typing.
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