Synthesis, alkaline phosphatase inhibition studies and molecular docking of novel derivatives of 4-quinolones

2017 ◽  
Vol 126 ◽  
pp. 408-420 ◽  
Author(s):  
Mariia Miliutina ◽  
Syeda Abida Ejaz ◽  
Shafi Ullah Khan ◽  
Viktor O. Iaroshenko ◽  
Alexander Villinger ◽  
...  
Keyword(s):  
Alkaline Phosphatase ◽  
Molecular Docking ◽  
Phosphatase Inhibition ◽  
Inhibition Studies ◽  
Derivatives Of ◽  
Alkaline Phosphatase Inhibition

Synthesis, Acetylcholinesterase and Alkaline Phosphatase Inhibition of Some New 1,2,4-Triazole and 1,3,4-Thiadiazole Derivatives

2012 ◽  
Vol 65 (10) ◽  
pp. 1413 ◽  
Author(s):  
Imtiaz Khan ◽  
Muhammad Hanif ◽  
Muhammad Tahir Hussain ◽  
Aftab Ahmed Khan ◽  
Muhammad Adil S. Aslam ◽  
...  
Keyword(s):  
Alkaline Phosphatase ◽  
Polyphosphoric Acid ◽  
Aqueous Sodium Hydroxide ◽  
Spectroscopic Studies ◽  
Standard Drug ◽  
1H And 13C Nmr ◽  
Phosphatase Inhibition ◽  
Thiosemicarbazide Derivatives ◽  
Inhibition Studies ◽  
Alkaline Phosphatase Inhibition

A new series of 4,5-disubstituted-2,4-dihydro-3H-1,2,4-triazole-3-thiones (6a–s) and 2,5-disubstituted-1,3,4-thiadiazoles (7a–h) was synthesized by intramolecular dehydrocyclization of various 1,4-disubstituted thiosemicarbazide derivatives (5a–s) by refluxing in 4 N aqueous sodium hydroxide and by overnight stirring with polyphosphoric acid, respectively. The structures of these compounds were characterized by IR, 1H and 13C NMR, elemental analysis and mass spectroscopic studies. All the synthesized compounds were screened for their acetylcholinesterase and alkaline phosphatase inhibition studies. Most of the tested compounds showed promising activities, amongst them (6k) and (6q) showed excellent acetylcholinesterase inhibitory activity with IC50 0.241 ± 0.012 and 0.260 ± 0.013 µM, respectively, as compared with those of standard drug whereas the compound (6p), with IC50 0.044 ± 0.001 µM, was found to be the most potent inhibitor of alkaline phosphatase.

Facile and expedient access to bis-coumarin–iminothiazole hybrids by molecular hybridization approach: synthesis, molecular modelling and assessment of alkaline phosphatase inhibition, anticancer and antileishmanial potential

RSC Advances ◽  
2015 ◽  
Vol 5 (109) ◽  
pp. 89919-89931 ◽  
Author(s):  
Aliya Ibrar ◽  
Sumera Zaib ◽  
Imtiaz Khan ◽  
Farukh Jabeen ◽  
Jamshed Iqbal ◽  
...  
Keyword(s):  
Alkaline Phosphatase ◽  
Molecular Modelling ◽  
Molecular Hybridization ◽  
Phosphatase Inhibition ◽  
Potential Inhibitors ◽  
Alkaline Phosphatase Inhibition

A series of new cytotoxic bis-coumarin–iminothiazole hybrids was developed as potential inhibitors of alkaline phosphatase and leishmaniasis.

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