56886-07-8Relevant articles and documents
Bis-heterocycles. Part I: Tetrahydro-5,5′- bi(1,2,4-triazin-6-ones)
Mohammad, Hanan H.,El-Abadelah, Mustafa M.,Sabri, Salim S.,Awwadi, Firas F.,Voelter, Wolfgang
, p. 965 - 974 (2018/11/23)
Selected sets of tetrahydro-5,5′-bi(1,2,4-triazines) (1-3) appended with acetyl, benzoyl, and ester moieties at C-3 position and N-1 (p-substituted)phenyl ring have been prepared and characterized by spectral (IR, NMR, MS) data and X-ray diffraction for c
Synthesis, in vitro and in Silico studies of some novel 5-nitrofuran-2-yl hydrazones as antimicrobial and antitubercular agents
Abdel-Aziz, Hatem Abdel-Kader,Eldehna, Wagdy Mohamed,Fares, Mohamed,Elsaman, Tilal,Abdel-Aziz, Marwa Mostafa,Soliman, Dalia Hussein
, p. 1617 - 1630 (2015/11/24)
In this study, we synthesized two series of novel 5-nitrofuran-2-carbohydrazides 21a-h and 22a-e in addition to a third series of thiophene-2-carbohydrazides 23a-g to develop potent antimicrobial and/or antitubercular agents. The newly synthesized compounds were evaluated in vitro for their antimicrobial and antimycobacterial activities. Most of the 5-nitrofuran-2-carbohydrazides 21a-h and 22a-e displayed variable activity against Aspergillus fumigates, Staphylococcus aureus, Streptococcus pneumonia, Bacillis subtilis, Salmonella typhimurium, Klebsiella pneumonia, Escherichia coli and Mycobacterium tuberculosis. The sulfonamide derivative 21f exhibited superior potency and broad-spectrum antimicrobial activity with minimum inhibitory concentration (MIC)=0.06-0.98 μg/mL and antimycobacterial activity with MIC=3.9 μg/mL. The 5-nitrofuran-2-carbohydrazides 21a, b, g, h and 22a-c exhibited significant antibacterial activity with MIC values in the range of 0.12-7.81 μg/mL. The significances of the 5-nitrofuran moiety and sulfonamide function were explored via the structure-activity relationship (SAR) study. In addition, docking studies revealed that the p-amino benzoic acid (PABA) and binding pockets of the dihydropteroate synthase (DHPS) were successfully occupied by compound 21f. Furthermore, two quantitative structure-activity relationship (QSAR) models were built to explore the structural requirements which controlled the activity.
Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
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Page/Page column 10-11, (2008/06/13)
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.