A new series of linked heterocyclics, 3-[4-(4-chlorophenyl)-6-(3,5-dimethyl-1-phenyl-1H-4-pyrazolyl)-2-pyrimidinyl]-2-(aryl/heteryl)-1,3-thiazolan-4-ones (6a-j), has been synthesized by the one-pot cyclo-condensation of 4-(4-chlorophenyl)-6-(3,5-dimethyl-1-phenyl-1H-4-pyrazolyl)-2-pyrimidinamine (5), aryl/heteroaryl aldehyde and thioglycolic acid. The structures of the synthesized compounds have been confirmed via IR, (1)H-NMR, (13)C-NMR, MS and elemental analyses. Further, all the newly synthesized compounds 6a-j have been assayed for their antimicrobial activity against Gram-positive and Gram-negative bacteria and fungi. The compounds containing moieties like 4-nitrophenyl (6c), 3-nitrophenyl (6d), 4-dimethylaminophenyl (6g), 2-furyl (6i) and 1,3-benzodioxole (6j), at 2-position of thiazolidin-4-one ring exhibited good inhibitory activity against all the tested organisms.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1248/cpb.58.1622 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Effect of Glycoconjugation on Cytotoxicity and Selectivity of 8-Aminoquinoline Derivatives Compared to 8-Hydroxyquinoline.
Molecules
January 2025
Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
Numerous emerging chemotherapeutic agents incorporate -heterocyclic fragments in their structures, with the quinoline skeleton being particularly significant. Our recent works have focused on glycoconjugates of 8-hydroxyquinoline (8-HQ), which demonstrated enhanced bioavailability and solubility compared to their parent compounds, although they fell short in selectivity. In this study, our objective was to improve the selectivity of glycoconjugates by replacing the oxygen atom with nitrogen by substituting the 8-HQ moiety with 8-aminoquinoline (8-AQ).
View Article and Find Full Text PDFBiomonitoring PhIP, a Potential Prostatic Carcinogen, in the Hair of Healthy Men of African and European Ancestry.
Toxics
January 2025
Masonic Cancer Center, Division of Pediatric Epidemiology and Clinical Research, University of Minnesota, Minneapolis, MN 55455, USA.
Heterocyclic aromatic amines (HAAs), formed during the cooking of meat, are potential human carcinogens, underscoring the need for long-lived biomarkers to assess exposure and cancer risk. Frequent consumption of well-done meats containing 2-amino-1-methyl-6-phenylimidazo[4,5-]pyridine (PhIP), a prevalent HAA that is a prostatic carcinogen in rodents and DNA-damaging agent in human prostate cells, has been linked to aggressive prostate cancer (PC) pathology. African American (AA) men face nearly twice the risk for developing and dying from PC compared to White men.
View Article and Find Full Text PDFInfluence of Drying Methods on the Morphological Features, Microstructural Properties, and Antioxidant Performance of : A Metabolomic Analysis.
J Fungi (Basel)
January 2025
State Key Laboratory of Plateau Ecology and Agriculture, Qinghai Academy of Animal and Veterinary Science, Xining 810016, China.
() has garnered increasing attention as an ingredient in both the pharmaceutical and food industries. Depending on the drying method, the accumulation of metabolites can greatly affect the quality. This research employed an untargeted metabolomics (LC-MS/MS) strategy to elucidate the similarities and differences in the morphological characteristics, microstructure, antioxidant capacity, and metabolic profiles of subjected to three distinct drying methods: natural air-drying (YG), oven-drying (HG), and vacuum freeze-drying (DG).
View Article and Find Full Text PDFDiving into Unknown Waters: Water-Soluble Clickable Au Nanoclusters Protected with N-Heterocyclic Carbenes for Bio-Medical Applications.
J Am Chem Soc
January 2025
Department of Chemistry, Queen's University, Chernoff Hall, Kingston, Ontario K7L 3N6, Canada.
The use of gold nanoclusters in biomedical applications has been steadily increasing in recent years. However, water solubility is a key factor for these applications, and water-soluble gold nanoclusters are often difficult to isolate and susceptible to exchange or oxidation in vivo. Herein, we report the isolation of N-heterocyclic carbene (NHC)-protected atomically precise gold nanoclusters functionalized with triethylene glycol monomethyl ether groups.
View Article and Find Full Text PDFDual VEGFR-2 and EGFR inhibitors of phenyldiazenes: anticancer evaluations, ADMET, docking, design and synthesis.
Future Med Chem
January 2025
Department of Chemistry, Faculty of Science, Ain Shams University, Cairo, Egypt.
Aim: New phenyldiazene scaffold-linked heterocyclic pyrazole, pyrimidinone, pyrimidinthione, and/or triazine rings have been developed and synthesized.
Methods & Results: Cytotoxicity of our derivatives was estimated on four cancer and VERO normal cell lines targeting EGFR (epidermal growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) enzymes. Our new derivatives selectively inhibited both VEGFR-2 and EGFR as they have the essential structural requirements for inhibitors of both receptors.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!