29246-90-0Relevant academic research and scientific papers
Design, synthesis and molecular docking of new N-4-piperazinyl ciprofloxacin-triazole hybrids with potential antimicrobial activity
Mohammed, Hamada H.H.,Abdelhafez, El-Shimaa M.N.,Abbas, Samar H.,Moustafa, Gamal A.I.,Hauk, Glenn,Berger, James M.,Mitarai, Satoshi,Arai, Masayoshi,Abd El-Baky, Rehab M.,Abuo-Rahma, Gamal El-Din A.
, (2019/05/01)
New N-4-piperazinyl ciprofloxacin-triazole hybrids 6a-o were prepared and characterized. The in vitro antimycobacterial activity revealed that compound 6a experienced promising antimycobacterial activity against Mycobactrium smegmatis compared with the reference isoniazide (INH). Additionally, compound 6a exhibited broad spectrum antibacterial activity against all the tested strains either Gram-positive or Gram-negative bacteria compared with the reference ciprofloxacin. Also, compounds 6g and 6i displayed considerable antifungal activity compared with the reference ketoconazole. DNA cleavage assay of the highly active compounds 6c and 6h showed a good correlation between the Mycobactrium cleaved DNA gyrase assay and their in vitro antimycobactrial activity. Moreover, molecular modeling studies were done for the designed ciprofloxacin derivatives to predict their binding modes towards Topoisomerase II enzyme (PDB: 5bs8).
An investigation of supramolecular synthons in 1,2,4-triazole-3(4H)-thione compounds. X-ray crystal structures, energetic and Hirshfeld surface analysis
Saeed, Aamer,Ashraf, Zaman,Nadeem, Humaira,Simpson, Jim,Pérez, Hiram,Erben, Mauricio F.
, p. 796 - 806 (2019/06/27)
A series of four closely related 1,2,4-triazole-3-thione (1-4) compounds was obtained by heterocyclization of thiosemicarbazides under basic catalytic conditions. The crystal structures of the 4-alkyl-5-(substituted-phenyl)-2H-1,2,4-triazole-3(4H)-thione
1,2,4-Triazole/oxime hybrids as new strategy for nitric oxide donors: Synthesis, anti-inflammatory, ulceroginicity and antiproliferative activities
Abuo-Rahma, Gamal El-Din A.A.,Abdel-Aziz, Mohamed,Beshr, Eman A.M.,Ali, Taha F.S.
, p. 185 - 198 (2014/01/06)
A series of novel nitric oxide (NO) donating triazole/oxime hybrids was prepared and evaluated for their anti-inflammatory activity and antiproliferative activity. Most of the tested compounds showed significant anti-inflammatory activity using carrageenan-induced rat paw edema method compared to indomethacin. Calculation of the ulcer indices and histopathological investigation indicated that the prepared NO-donating oximes exhibited less ulcerogenicity compared to their ketone intermediates and indomethacin. The NO-donating oximes 7i and 7k achieved remarkable cell growth inhibition activity against most of the tested cell lines. Compound 7k was found to be with high selectivity against CNS subpanel with selectivity ratio of 11.99 at GI 50 level.
New nitric oxide donating 1,2,4-triazole/oxime hybrids: Synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities
Abdel-Aziz, Mohamed,Abuo-Rahma, Gamal El-Din A.A.,Beshr, Eman A.M.,Ali, Taha F.S.
, p. 3839 - 3849 (2013/07/19)
A series of novel nitric oxide (NO) donating triazole/oxime hybrids was prepared and evaluated for their anti-inflammatory activity. Most of the tested compounds showed significant anti-inflammatory activity using carrageenan-induced rat paw edema method compared to indomethacin. Calculation of the ulcer indices and histopathological investigation indicated that the prepared NO-donating oximes exhibited less ulcerogenicity compared to their intermediate ketones and indomethacin. The NO-donating oxime 6i revealed significant activity against renal cancer A498 cell lines with 50.52 cell growth inhibition.
1,3,4-Thiadiazoles. Regioselective O-demethylation on dehydrative cyclization of 1-(3,4,5-trimethoxybenzoyl)-4-substituted thiosemicarbazides with sulphuric acid
Al-Omar, Mohamed,Al-Deeb, Omar A.,Al-Khamees, Hamad A.,El-Emam, Ali A.
, p. 2509 - 2517 (2007/10/03)
Cyclization of 1-(3,4,5-trimethoxybenzoyl)-4-substituted thiosemicarbazides 2a-g with sulphuric acid at ambient temperature afforded the selectively demethylated products 2-(4-hydroxy-3,5-dimethoxyphenyl)-5-substituted amino-1,3,4-thiadiazoles 4a-g. Meanw
