193826-40-3Relevant articles and documents
Design and synthesis of new benzylidene-quinazolinone hybrids as potential anti-diabetic agents: In vitro α-glucosidase inhibition, and docking studies
Ayyad, Rezk R.,Ibrahim, Albaraa,Khalifa, Mohamed M.,Mansour, Ahmed M.,Sakr, Helmy M.
, (2021/11/08)
A novel series of benzylidene-quinazolinone hybrids 8a,b and 10a-n were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory effect aiming to discover efficient anti-diabetic agents. The synthesized compounds were assessed for their in vivo anti-hyperglycemic activities against STZ-induced hyperglycemic rats. Five compounds (10m, 10f, 10c, 10d and 8b) demonstrated potent activities with percent reduction in blood glucose levels of 43.07, 40.14, 39.83, 37.04 and 36.16, respectively. The most active members were further evaluated in vitro for their α-glucosidase inhibitory binding affinities. Among them, Compound 10m containing 4-hydroxybenzylidene moiety and compound 10f with 4-chlorobenzylidene moiety connected to the acetohydrazide demonstrated the most potent inhibitory activities towards α-glucosidase with IC50 values of 561 and 610 μM, respectively. Molecular docking study was performed in order to understand the molecular interactions between the molecule and enzyme.
New scaffold of 4-oxo-thiazolidine derivatives as potent anti-infective agents
Godhani, Dinesh R.,Jogel, Anand A.,Sanghani, Anil M.,Mehta, Jignasu P.
, p. 734 - 746 (2017/01/18)
A new series of 4-oxo-thiazolidine has been synthesized and compounds 5a-j have been characterized by various techniques like FT-IR, 1H and 13C NMR, and mass spectroscopy. All the newly synthesized compounds have been screened against four bacterial strains: Staphylococcus aureus, Streptococcus pyogenus, Escherichia coli, Pseudomonas aeruginosa and two fungal pathogens: Candida albicans and Aspergillus clavatus. The results have been expressed as minimal inhibition concentration (MIC μg/mL) in comparison with standard drugs. Compounds 5a, 5c, 5d, 5e, and 5i show moderate to good activity against selected bacterial strains (MIC = 62.5 μg/mL to 125 μg/mL). In vitro antitubercular activity study of newly synthesized compounds 5a-j has been carried out against Mycobacterium tuberculosis H37Rv. Two compounds 5c and 5j have shown good antituberculosis activity in comparison with standard drugs.
Synthesis of some New 2-Thioxoquinazolin-4-ones
Deshmukh,Deshmukh,Shirke
, p. 422 - 423 (2007/10/03)
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