36974-48-8Relevant academic research and scientific papers
Catalytic Asymmetric Synthesis of anti-α,β-Diamino Acid Derivatives
Izumi, Sanae,Kobayashi, Yusuke,Takemoto, Yoshiji
, p. 696 - 699 (2016)
A novel approach to chiral anti-α,β-diamino acid derivatives through tandem orthogonal organocatalysis has been developed. Chiral phosphoric acid catalysts control the chemo-, regio-, and stereoselective addition of hydroxylamines to alkylideneoxazolones, while a phosphine catalyst promotes the isomerization of Z- alkylideneoxazolones to the more reactive E- alkylideneoxazolones. (Chemical Equation Presented).
Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation
Aboeldahab, Alshimaa M.A.,Beshr, Eman A.M.,Shoman, Mai E.,Rabea, Safwat M.,Aly, Omar M.
, p. 79 - 92 (2018)
Two structurally novel series of histone deacetylase inhibitors (HDACIs) involving two potential surface recognition moieties; 3′,4′-dihydro-2′H-spiro[imidazolidine-4,1′-naphthalene]-2,5-dione (in series I) and 1-(3-methoxyphenyl)-5-(3,4,5-trimethoxypheny
Synthesis, cytotoxicity, docking study, and tubulin polymerization inhibitory activity of novel 1-(3,4-dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)- 1h-1,2,4-triazole-3-carboxanilides
Aly, Omar M.,Beshr, Eman A.,Maklad, Raed M.,Mustafa, Muhamad,Gamal-Eldeen, Amira M.
, p. 658 - 667 (2014)
A series of novel 1-(3,4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2, 4-triazole-3-carboxylic acid derivatives (4a-n) were synthesized and evaluated for their in vitro cytotoxic activity against the growth of four different human cell lines (hepatoca
Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study
Mustafa, Muhamad,Anwar, Sirajudheen,Elgamal, Firgani,Ahmed, Esam R.,Aly, Omar M.
, (2019)
A series of cis restricted 1,2,4-triazole analogs of combretastatin A-4 (CA-4) were designed and synthesized. The antiproliferative activity of these compounds was measured on hepatocellular carcinoma HepG2, leukemia HL-60, and breast cancer MCF-7 cell li
Design, synthesis, anticonvulsant activity, and pharmacophore study of new 1,5-diaryl-1H-1,2,4-triazole-3-carboxamide derivatives
Abuelhassan, Abdelfattah H.,Badran, Mostafa M.,Hassan, Heba A.,Abdelhamed, Dalia,Elnabtity, Sameh,Aly, Omar M.
, p. 928 - 938 (2017/11/27)
1,5-Diaryl-1H-1,2,4-triazole-3-carboxamide derivatives were designed, synthesized, and evaluated for its anticonvulsant activity using maximal electroshock (MES) and chemoshock (scPTZ and Strychnine) animal screen methods. Neurotoxicity was also assessed. In MES model, compound 4f showed 100% of phenytoin activity after both 0.5 and 4 h. In scPTZ model, compound 4e showed 100% of sodium valproate activity. In Strychnine model, compound 4e showed 120% more delay of onset of convulsion and 124% more delay of time of death relative to sodium valproate. Most of the target compounds showed mild neurotoxicity especially compound 4f which showed excellent activity against electroshock. Pharmacophoric study reveals that the synthesized compounds showed good fitting on the pharmacophoric query with good RMSDX results.
Synthesis, cytotoxicity, and docking study of novel 1-naphthyl-5-aryl-1H-1,2,4-triazole-3-carboxamides
Zaki, Islam,Ramadan, Mohamed,Abdelrahman, Mostafa H.,Aly, Omar M.
, p. 1483 - 1496 (2017/07/18)
A new series of 1-naphthyl-5-aryl-1H-1,2,4-triazole-3-carboxamide derivatives were synthesized and structurally proved by 1H and 13C NMR along with high-resolution mass spectrometry. The cytotoxic activity of the newly synthesized compounds was evaluated. Compounds showed a pronounced inhibitory effect against cellular localization of tubulin. Flow cytometric analysis showed that Hep-G2 cells treated indicated a predominated growth arrest at the G2/M-phase compared to that of S-phase. Molecular modeling study using MOE program indicated that most of the target compounds showed good binding with the colchicine-binding site of β-subunit of tubulin with the binding free energy (?G) values of about 42?kJ/mol. Graphical abstract: [Figure not available: see fulltext.].
1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3- carboxamides: Synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity
Abdel-Aziz, Mohamed,Beshr, Eman A.,Abdel-Rahman, Islam M.,Ozadali, Keriman,Tan, Oya Unsal,Aly, Omar M.
, p. 155 - 165 (2014/04/03)
A series of novel 1-(4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4- triazole-3-carboxamides were synthesized and confirmed with different spectroscopic techniques. The prepared compounds exhibited remarkable anti-inflammatory activity that represen
