18440-55-6Relevant academic research and scientific papers
Synthesis and cytotoxic activity study of novel 2-(Aryldiazenyl)-3-methyl-1h-benzo[g]indole derivatives
Abdel-Jalil, Raid J.,Adham, Sirin A. I.,Arafeh, Manar M.,Moghadam, Ebrahim Saeedian,Stoll, Raphael
, (2021/07/26)
A novel series of 2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives (3a–f) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (3a–f) were characterized using1H NMR,13C NMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 μM concentration, two of them (2c) and (3c) were subjected to five dose screens and showed a significant cytotoxicity and selectivity.
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
Spectral characterization, CT-DNA binding, DFT/B3LYP, molecular docking and antitumor studies for new nano-sized VO(II)-hydrazonoyl complexes
Althagafi, Ismail,Elghalban, Marwa G.,Saad, Fawaz,Al-Fahemi, Jabir H.,El-Metwaly, Nashwa M.,Bondock, Samir,Almazroai, Layla,Saleh, Kamel A.,Al-Hazmi, Gamil A.
, p. 662 - 677 (2017/07/27)
New hydrazonoyl chloride derivatives were prepared and characterized. Their VO(II) complexes were isolated after adjusting reaction medium to slightly basic by 0.5?g acetate. Neutral tridentate mode is a general coordination feature of ligands towards bin
Synthesis and fluorescent behaviour of 2-aryl-4,5-dihydro-1H-1,2,4-triazoles
Eliseeva, Alexandra I.,Nesterenko, Olga O.,Slepukhin, Pavel A.,Benassi, Enrico,Belskaya, Nataliya P.
, p. 86 - 100 (2017/04/01)
A series of new 4,5-dihydro-1H-1,2,4-triazoles was synthesized from amidrazones and acetylenedicarboxylic acid esters in the presence of pyridine in toluene. The synthesized compounds were characterized by 1H, 13C NMR, FT-IR spectral analyses and XRD data
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).
