78077-47-1Relevant academic research and scientific papers
Synthesis and structure-activity relationship; exploration of some potent anti-cancer phenyl amidrazone derivatives
Habashneh, Almeqdad Y.,El-Abadelah, Mustafa M.,Bardaweel, Sanaa K.,Taha, Mutasem O.
, p. 468 - 477 (2018/07/25)
Background: Amidrazones have been reported to have significant anti-tumor properties against several cancer cell lines. Objectives: The current project aims to profile the structure-anticancer activity relationship of phenyl-amidrazons. Methods: Fifteen p
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.
Metal-assisted oxidative cyclization of arylamidrazones II [1]. Novel synthesis of 1,4-diaryi[1,2,4]triazino[6,5-h]quinolines
Khanfar, Monther A.,Abu Thaher, Bassam A.,Zahra, Jalal A.,Al-Qawasmeh, Raed A.,El-Abadelah, Mustafa M.,Voelter, Wolfgang
experimental part, p. 1107 - 1111 (2009/05/30)
New model 1,2,4-triazino[6,5-h]quinolines 8a-c are prepared by oxidative cyclization of the respective N-(quinolin-8-yl)amidrazone precursors 7a - c using copper(II) chloride. Interestingly, the cyclized products 8a - c were found to be arylated at N1posi
Reaction of nitrilimines with alkoxycarbonyl-hydrazines: Synthesis of 6-acetyl-4-aryl-2-ethoxycarbonyl-1,2,3,4-tetrahydro-s-tetrazines
El-Haddad, Mihtab R.,Ferwanah, Abed El-Rahman S.,Awadallah, Adel M.
body text, p. 623 - 626 (2011/10/13)
Nitrilimines 2 are found to react with alkoxycarbonylhydrazines 3-5 to afford the acyclic adducts 6-8. 6c is oxidized upon heating with charcoal in refluxing toluene to the corresponding formazan 9c. Compounds 8 cyclize upon heating with charcoal in reflu
HETEROCYCLES FROM NITRILE IMINES. PART IV. CHIRAL 4,5-DIHYDRO-1,2,4-TRIAZIN-6-ONES
El-Abadelah, Mustafa M.,Hussein, Ahmad Q.,Thaher, Bassam A.
, p. 1879 - 1895 (2007/10/02)
The reaction of nitrile imines (II) with α-amino esters (III) proceeds with no detectable racemization and constitutes a convenient synthetic route to 4,5-dihydro-1,2,4-triazin-6-ones (IV).Permangamate oxidation of heterocycles (IV) affords the corresponding 1,2,4-triazin-6-ones (V).The reaction of (II) with β-amino esters gives the respective acyclic amidrazone adducts (VI).
