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Inhibitory Effects of Sulfur Derivatives on Cell Viability and Secreted Acid Phosphatase In Vitro.
Microorganisms
December 2024
Department of Chemistry, Illinois State University, Normal, IL 61790, USA.
Sulfonamide drugs were the original class of antibiotics, demonstrating the antibacterial potential of dithiocarbazate and thiosemicarbazone Schiff base derivatives of syringaldehyde and 4-hydroxy-3,5-dimethylbenzaldehyde. We synthesized unique Schiff bases via the condensation of the aldehydes with hydrazine derivatives, which allows for the easy synthesis of several related compounds. These Schiff base derivatives were tested for antileishmanial properties against the parasitic protozoan .
View Article and Find Full Text PDFDesign, Synthesis, Antimicrobial Activity, and Molecular Docking of Novel Thiazoles, Pyrazoles, 1,3-Thiazepinones, and 1,2,4-Triazolopyrimidines Derived from Quinoline-Pyrido[2,3-] Pyrimidinones.
Pharmaceuticals (Basel)
December 2024
Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623, Saudi Arabia.
Background: Recently, pyrido[2,3-] pyrimidine, triazolopyrimidine, thiazolopyrimidine, quinoline, and pyrazole derivatives have gained attention due to their diverse biological activities, including antimicrobial, antioxidant, antitubercular, antitumor, anti-inflammatory, and antiviral effects.
Objective: The synthesis of new heterocyclic compounds including 5-quinoline-pyrido[2,3-] pyrimidinone (-, , -), 6-quinoline-pyrido[2,3-]thiazolo[3,2-]pyrimidinone (, , -), 1,2,4-triazole-6-quinoline-pyrido[2,3-]thiazolo[3,2-]pyrimidinone (-), and pyrido[2,3-]thiazolo[3,2-]pyrimidine-ethyl-(pyridine)-9-thiaazabenzo[]azulenone () derivatives was performed with high yields while evaluating antimicrobial activities.
Methods: A new series of quinoline-pyrido[2,3-]thiazolo[3,2-]pyrimidine derivatives were prepared using a modern style and advanced technology, resulting in high yields of these new compounds.
Novel Antimicrobial and Antitumor Agents Bearing Pyridine-1,2,4-triazole-3-thione-hydrazone Scaffold: Synthesis, Biological Evaluation, and Molecular Docking Investigation.
Biomolecules
November 2024
Department of Organic Chemistry, Kaunas University of Technology, Radvilėnų pl. 19, 50254 Kaunas, Lithuania.
A series of target 4-substituted-5-(2-(pyridine-2-ylamino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thiones and their chloro analogs - were synthesized in a reaction of the selected aldehydes with the corresponding 4-amino-1,2,4-triazole-3-thiones and , which were obtained from 3-(pyridin-2-ylamino)propanoic acid () or 3-((5-chloropyridin-2-yl)amino)propanoic acid (), respectively, with thioacetohydrazide. The antibacterial and antifungal activities of the synthesized hydrazones were screened against the bacteria , , and and the fungi and by agar diffusion and serial dilution methods. 4-Amino-5-(2-((5-chloropyridin-2-yl)amino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thione () and 4-(benzylideneamino)-5-(2-(pyridin-2-ylamino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thione () were identified as exceptionally active (MIC 0.
View Article and Find Full Text PDFHarnessing acylhydrazone-oxime exchange reaction to achieve diverse synthesis of glycosite-specific antibody-drug conjugates.
Org Biomol Chem
January 2025
School of Pharmaceutical Science and Technology, Hangzhou Institute of Advanced Study, Hangzhou 310024, China.
Glycosite-specific antibody-drug conjugates (gsADCs), which carry cytotoxic payloads at the conserved -glycosylation site, N297, of an IgG, have emerged as a promising ADC format with better therapeutic index. Conjugating the payloads aldehyde-based chemistry is more friendly to IgGs, and has been widely investigated. However, the efficiency of introducing an aldehyde tag at the N297 site is poor due to the complicated procedures required, such as the multiple-enzyme-catalyzed IgG glycoengineering process and the successive oxidation step, which always results in heterogeneous products and poor stability.
View Article and Find Full Text PDFExploring pyrazolines as potential inhibitors of NSP3-macrodomain of SARS-CoV-2: synthesis and in silico analysis.
Sci Rep
January 2025
Bioinformatics Centre, Savitribai Phule Pune University, Pune, Maharashtra, 411007, India.
COVID-19 has proved to be a global health crisis during the pandemic, and the emerging JN.1 variant is a potential threat. Therefore, finding alternative antivirals is of utmost priority.
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