38407-30-6Relevant articles and documents
Semicarbazone derivatives as urease inhibitors: Synthesis, biological evaluation, molecular docking studies and in-silico ADME evaluation
Qazi, Syeda Uroos,Rahman, Shafiq Ur,Awan, Asia Naz,al-Rashida, Mariya,Alharthy, Rima D.,Asari, Asnuzilawati,Hameed, Abdul,Iqbal, Jamshed
, p. 19 - 26 (2018/05/14)
A series of hydrazinecarboxamide derivatives were synthesized and examined against urease for their inhibitory activity. Among the series, the 1-(3-fluorobenzylidene)semicarbazide (4a) (IC50 = 0.52 ± 0.45 μM), 4u (IC50 = 1.23 ± 0.32 μM) and 4h (IC50 = 2.22 ± 0.32 μM) were found most potent. Furthermore, the molecular docking study was also performed to demonstrate the binding mode of the active hydrazinecarboxamide with the enzyme, urease. In order to estimate drug likeness of compounds, in silico ADME evaluation was carried out. All compounds exhibited favorable ADME profiles with good predicted oral bioavailability.
New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease
Pizzo, Chiara,Faral-Tello, Paula,Yaluff, Gloria,Serna, Elva,Torres, Susana,Vera, Ninfa,Saiz, Cecilia,Robello, Carlos,Mahler, Graciela
, p. 107 - 113 (2016/01/15)
Herein, we describe a new approach towards the synthesis of selenosemicarbazones. The reaction involves an O-Se exchange of semicarbazones using Ishihara reagent. Eleven selenosemicarbazones were prepared using this methodology, with low to moderate yields. Among the prepared compounds the m-bromo phenyl methyl derivative 1b was selected to be evaluated in vivo, in a murine model of acute Chagas' disease. Compound 1b 10 mg/kg bw/day reduced 50% of parasitaemia profile compared with the control group, but was less effective than Benznidazole (50 mg/kg bw/day reduced 90%) and toxic. These studies are important to guide future Chagas drug design.
Microwave assisted synthesis and characterization of semicarbazones
Jadon, Sudha,Khedr, Abdalla M.,Kumar, Sanjeev,Yadav, Sneha,Kumar, Vipin,Gupta, Kishan C.
experimental part, p. 4209 - 4211 (2012/01/04)
An efficient and simple microwave assisted procedure has been developed for conversion of substituted aryl aldehyde to corresponding semicarbazone by reaction with semicarbazide hydrochloride in presence of sodium acetate. The synthesized semicarbazones have been characterized by physico-chemical and spectral data.