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Discovery of Novel Thiazolohydrazone Derivatives as an Alternative Option in the Treatment of Zoonotic Toxocara canis: In Vitro and In Silico Evaluation.
Vet Med Sci
January 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
Thiazoles serve as pharmacophores in many molecules that exhibit significant biological activity. This study used in vitro assays and in silico methodologies to identify novel medication candidates for preclinical evaluation of visceral toxocariasis treatment. The objective was to assess the impact of 11 thiazolohydrazone derivative compounds on the larval eggs of Toxocara canis.
View Article and Find Full Text PDFInhibitory 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 PDFClinical predictors of 3-month isoniazid rifapentine (3HP)-related adverse drug reactions (ADR) during tuberculosis preventive therapy (PAnDoRA-3HP study): an observational study protocol.
BMJ Open
December 2024
Infectious Diseases Institute, Makerere University College of Health Sciences, Kampala, Central, Uganda.
Introduction: Tuberculosis (TB) is the leading infectious cause of death globally. Despite WHO recommendations for TB preventive therapy (TPT), challenges persist, including incompletion of treatment and adverse drug reactions (ADRs). There is limited data on the 3-month isoniazid and rifapentine (3HP) pharmacokinetics, pharmacogenomics and their relation with ADRs.
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