- Antimicrobial Activity of N-(3-Chloro-2-aryl-4-oxoazetidin-1-yl)-4-nitro benzamide Derivatives
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A series of N-(3-chloro-2-aryl-4-oxoazetidin-1-yl)-4-nitro benzamide derivatives (4a-g) were synthesized by reacting various N’-arylidene-4-nitro benzo hydrazide (3a-g) with chloro acetyl chloride in the presence of triethylamine and dioxane. Infrared (IR), proton nuclear magnetic resonance (1HNMR), and mass (MS) spectrometric techniques were used to describe the structure of synthesized compounds, which were further tested for in vitro antibacterial activity, and benzylpenicillin was used as a reference drug. Compounds (4b) and (4e) were showed high antibacterial action, whereas the remaining compounds (4a, 4c, 4d, 4f, and 4g) were showed moderate activity. Finally, this research demonstrates the design and development of novel antibacterial agents.
- Alghamdi, Saad,Almehmadi, Mazen M.,Asif, Mohammad
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- 3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles: A new scaffold for the selective inhibition of monoamine oxidase B
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3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles were designed, synthesized, and tested as inhibitors against human monoamine oxidase (MAO) A and B isoforms. Several compounds, obtained as racemates, were identified as selective MAO-B inhibitors. The enantiomers of some derivatives were separated by enantioselective HPLC and tested. The R-enantiomers always showed the highest activity. Docking study and molecular dynamic simulations demonstrated the putative binding mode. We conclude that these 1,3,4-oxadiazoles derivatives are promising reversible and selective MAO-B inhibitors.
- MacCioni, Elias,Alcaro, Stefano,Cirilli, Roberto,Vigo, Sara,Cardia, Maria Cristina,Sanna, Maria Luisa,Meleddu, Rita,Yanez, Matilde,Costa, Giosuè,Casu, Laura,Matyus, Peter,Distinto, Simona
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experimental part
p. 6394 - 6398
(2011/11/06)
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- Lewis acid-mediated nucleophilic addition of dialkylphosphite to C=N double bond of hydrazones
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The synthesis of new phenyl substituted derivatives (2) of -hydrazino-alkylphosphonic acids by Lewis acid-mediated addition of dialkylphosphite to hydrazones, derived from benzoylhydrazines and benzaldehydes, is described. Reactions were successfully prom
- Lien, Chia-Ling,Yeh, Shu-Hua,Hsu, Chi-Tung
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experimental part
p. 543 - 549
(2009/11/30)
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- Synthesis of some novel pharmacologically active schiff bases using microwave method and their derivatives formazans by conventional method
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Condensation of p-nitrobenzoylhydrazide 1 with substituted aromatic aldehydes 2 under microwave irradiation and by conventional method provide Schiff bases 3a-j. Schiff bases 3a-j on condensation with diazonium salt of 6-methoxy-2-aminobenzothiazole give formazans 4a-j. This reaction is carried out only by conventional method.
- Desai, Krunal G.,Desai
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p. 2097 - 2101
(2007/10/03)
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