351980-45-5Relevant academic research and scientific papers
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.
Synthesis and antiviral activity of new substituted methyl [2-(arylmethylene-hydrazino)-4-oxo-thiazolidin-5-ylidene]acetates
Saeed, Aamer,Al-Masoudi, Najim A.,Latif, Muhammad
, p. 618 - 625 (2013/09/02)
A series of new methyl [2-(arylmethylene-hydrazono)-4-oxo-thiazolidin-5- ylidene]acetates (5a-o) were synthesized via cyclocondensation of thiosemicarbazones (3a-o) with dimethyl but-2-ynedioate (4) in good yields under solvent-free conditions. The environmentally friendly solvent-free protocol overcomes the limitations associated with the customary protracted solution phase synthesis and afforded the title compounds in a few minutes. Compounds 5b-i and 5h-o were evaluated for their antiviral activity against the replication activity of HIV-1 and HIV-2 in MT-4 using the MTT assay. The same compounds were also evaluated in vitro for their selective antiviral activity against hepatitis C virus (HCV) in the Huh 5-2 replicon system (type 1b, Con1 strain).
Green synthesis of 2-amino-5-substituted-1,3,4-oxadiazoles at the platinum anode in acetic acid
Sharma, Laxmi Kant,Singh, Sushma,Singh
experimental part, p. 110 - 114 (2011/04/15)
The electroorganic synthesis of 2-amino-5-substituted-1,3,4-oxadiazoles from the anodic oxidation of semicarbazone has been carried out at platinum anode in acetic acid under constant potential electrolysis in an undivided cell. This is an environmentally benign method in the field of synthetic organic chemistry. The products are characterized by IR, 1H and 13C NMR, and elemental analysis.
