A new series of fused pyran derivatives 5a-x bearing 2-morpholinoquinoline nucleus has been synthesized under microwave irradiation by a reaction of 2-morpholinoquinoline-3-carbaldehyde 2a-c, malononitrile 3 and compounds 4a-h in presence of NaOH as basic catalyst. All the compounds were screened against three Gram positive bacteria (Streptococcus pneumoniae, Clostridium tetani, Bacillus subtilis), three Gram negative bacteria (Salmonella typhi, Vibrio cholerae, Escherichia coli) and two fungi (Aspergillus fumigatus, Candida albicans) using broth microdilution MIC (Minimum Inhibitory Concentration) method. Of the compounds studied, compounds 5b, 5f, 5k, 5m, 5q, 5s and 5v have found to be most efficient members of the series.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2011.07.123 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Bicyclic polyprenylated acylphloroglucinol-related meroterpenoids as potent DRAK2 inhibitors from Hypericum patulum.
Phytochemistry
December 2024
Shanghai Frontiers Science Center of Drug Target Identification and Delivery, School of Pharmaceutical Sciences, Shanghai Jiao Tong University, Shanghai, 200240, China; School of Pharmacy, Fudan University, Shanghai, 201203, China. Electronic address:
As a both edible and medicinal plant, Hypericum patulum (Hypericaceae) is used as a natural herbal tea, scented tea, and folk medicine. In this study, eight undescribed bicyclic polyprenylated acylphloroglucinol-related meroterpenoids named hyperpatins A-H, along with eight known ones, were isolated from this plant. Their structures were elucidated on the basis of spectroscopic techniques, chemical method, X-ray crystallographic experiments, and electronic circular dichroism analyses.
View Article and Find Full Text PDF2-Amino-5-oxo-4-(thio-phen-2-yl)-5,6,7,8-tetra-hydro-4-chromene-3-carbo-nitrile.
IUCrdata
November 2024
School of Chemistry and Physics, University of KwaZulu-Natal, Westville campus, Private bag X54001, Durban, 4000, South Africa.
The crystal structure of the title compound, CHNOS, reveals two symmetrically independent mol-ecules within the asymmetric unit. Each mol-ecule contains a chromenone core attached to a 2-thio-phene ring, cyano, and amino groups. The 2-thio-phene ring of one of the two mol-ecules in the asymmetric unit was found to be disordered over two positions, with the major component having a site occupancy factor of 0.
View Article and Find Full Text PDFTherapeutic Contribution of Tau-Binding Thiazoloflavonoid Hybrid Derivatives Against Glioblastoma Using Pharmacological Approach in 3D Spheroids.
Int J Mol Sci
November 2024
Faculté des Sciences Médicales et Paramédicales, Institut de Neurophysiopathologie (INP), UMR 7051, CNRS, Aix Marseille Université, 13005 Marseille, France.
Growing evidence has unveiled the pathological significance of Tau in many cancers, including the most aggressive and lethal brain tumor glioblastoma multiform (GBM). In this regard, we have recently examined the structure-activity relationship of a new series of seventeen 2-aminothiazole-fused to flavonoid hybrid compounds (TZF) on Tau-overexpressing GBM cells. Here, we evaluated the anticancer activities of the two lead compounds and using multi-cellular spheroids (MCSs) which represent an easy 3D human cell model to mimic GBM organization, physical constraints and drug penetration.
View Article and Find Full Text PDFRecombinant bovine serum albumin domain II as bioreceptor for ochratoxin A capture.
Talanta
February 2025
CEB - Centre of Biological Engineering, University of Minho, 4710-057, Braga, Portugal; LABBELS - Associate Laboratory, Braga/Guimarães, Portugal. Electronic address:
Established chromatographic techniques for mycotoxin control in foodstuffs require prior sample enrichment and clean-up, typically achieved using immunoaffinity columns (IACs). Bovine serum albumin (BSA) has recently emerged as a cost-effective alternative to antibodies used in IACs. This study aimed at exploring the BSA domain II (BDII), which houses the primary binding site for ochratoxin A (OTA), as a bioreceptor for OTA capture.
View Article and Find Full Text PDFNovel compound, pleuropyronine, and other polyketides isolated from the edible mushroom Pleurotus ostreatus suppress bacterial biofilm formation.
Biosci Biotechnol Biochem
December 2024
Novel Compounds Exploration Research Organization, Tsukuba, Japan.
An increase in the number of drug-resistant microbes is a major threat to human health. Bacterial drug resistance is mostly mediated by biofilm formation. In this study, the culture filtrate from the edible mushroom, Pleurotus ostreatus, was fractionated to isolate compounds that inhibit the biofilm formation of six pathogenic bacteria.
View Article and Find Full Text PDFWant 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!