Pyrazole and Nicotinonitrile Derivatives Synthesized from Sulfa Drugs, and Their Antibacterial Activity
- 作者: El-Sayed H.1, Moustafa A.1, Fadda A.1, Abd El-Rahman K.1
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隶属关系:
- Department of Chemistry, Faculty of Science
- 期: 卷 89, 编号 2 (2019)
- 页面: 339-347
- 栏目: Article
- URL: https://journals.rcsi.science/1070-3632/article/view/222769
- DOI: https://doi.org/10.1134/S1070363219020270
- ID: 222769
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详细
Utility of sulfadiazine and sulfaguanidine in synthesis of new series of pyrazoles and 2-pyridones is described. Diazotization of sulfadiazine that results in formation of diazonium salt 2 followed by coupling of the latter with active methylene compounds leads to hydrazinyl derivatives 3a–3d. Heterocyclization of compounds 3a–3c with hydrazine derivatives gives to a series of pyrazole derivatives 4–6. Similarly, a series of pyrazole derivatives 12–14 is developed from sulfaguanidine. Condensation of hydrazinyl derivatives 3a–3c with cyanoacetamide in the presence of a catalytic amount of piperidine gives 2-oxonicotinonitriles 15a–15c. Tests of the new synthesized compounds against four pathogenic gram (+ve) and gram (−ve) bacteria demonstrate their activity higher than that of the standard Amoxicillin.
作者简介
H. El-Sayed
Department of Chemistry, Faculty of Science
编辑信件的主要联系方式.
Email: hasanneg@gmail.com
埃及, Zagazig, 44519
A. Moustafa
Department of Chemistry, Faculty of Science
Email: hasanneg@gmail.com
埃及, Zagazig, 44519
A. Fadda
Department of Chemistry, Faculty of Science
Email: hasanneg@gmail.com
埃及, Mansoura
K. Abd El-Rahman
Department of Chemistry, Faculty of Science
Email: hasanneg@gmail.com
埃及, Zagazig, 44519