75322-50-8Relevant academic research and scientific papers
An Efficient Greener Approach for N-acylation of Amines in Water Using Benzotriazole Chemistry
Ibrahim, Tarek S.,Seliem, Israa A.,Panda, Siva S.,Al-Mahmoudy, Amany M.M.,Abdel-Samii, Zakaria K.M.,Alhakamy, Nabil A.,Asfour, Hani Z.,Elagawany, Mohamed
, (2020/06/17)
A straightforward, mild and cost-efficient synthesis of various arylamides in water was accomplished using versatile benzotriazole chemistry. Acylation of various amines was achieved in water at room temperature as well as under microwave irradiation. The developed protocol unfolds the synthesis of amino acid aryl amides, drug conjugates and benzimidazoles. The environmentally friendly synthesis, short reaction time, simple workup, high yields, mild conditions and free of racemization are the key advantages of this protocol.
Synthesis and antitubercular evaluation of N-Arylpyrazine and N,Na-Alkyl-diylpyrazine-2-carboxamide derivatives
Bispo, Marcelle De Lima Ferreira,Goncalves, Raoni Schroeder Borges,Lima, Camilo Henrique Da Silva,Cardoso, Laura Nogueira De Faria,Lourenco, Maria Cristina Silva,De Souza, Marcus Vinicius Nora
, p. 1317 - 1322 (2013/02/22)
Two series of pyrazinamide (PZA) derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Some compounds exhibited minimum inhibitory concentration activity of 50-100 μg/mL, greater than the first line antituberculosis drug PZA in Alamar Blue assay (>100 μg/mL). The obtained activities can be considered promising results, which characterizes these compounds as good start points to development of new antitubercular agents.
Synthesis and antimycobacterial evaluation of substituted pyrazinecarboxamides
Dolezal, Martin,Cmedlova, Pavlina,Palek, Lukas,Vinsova, Jarmila,Kunes, Jiri,Buchta, Vladimir,Jampilek, Josef,Kralova, Katarina
, p. 1105 - 1113 (2008/09/20)
Unsubstituted, halogenated and/or alkylated pyrazine-2-carboxylic acid amides connected via -CONH- bridge with substituted anilines were synthesized using currently known synthetic pathways. The synthetic approach, analytical, spectroscopic, lipophilicity and biological data of 20 newly synthesized compounds are presented. Structure-activity relationships among the chemical structures, the antimycobacterial, antifungal, photosynthesis inhibiting and antialgal activity of the evaluated substituted N-phenylpyrazine-2-carboxamides are discussed. 5-tert-Butyl-6-chloro-N-(3-trifluoromethylphenyl)pyrazine-2-carboxamide (19) has shown the highest activity against Mycobacterium tuberculosis H37Rv (MIC = 3.13 μg/mL). The highest antifungal effect against Trichophyton mentagrophytes, the most susceptible fungal strain tested, was found for N-(3-trifluoromethylphenyl)pyrazine-2-carboxamide (14, MIC = 62.5 μmol/mL). The highest reduction of chlorophyll content in Chlorella vulgaris was found for pyrazine-2-carboxylic acid (3-trifluoromethylphenyl)amide (9, IC50 = 12.1 μmol/L).
Heteroacyl Azides as Acylating Agents for Aromatic or Heteroatomic Amines (1)
Stanovnik, B.,Tisler, M.,Golob, V.,Hvala, I.,Nikolic, O.
, p. 733 - 736 (2007/10/02)
The possibility of formation of substituted heterocyclic amides from heteroacyl azides and aromatic or heteroatomic amines was investigated.Although acylation proceeded in some cases under mild reaction conditions, formation of N,N'-disubstituted ureas was the main process at elevated temperatures.
