Vinsova_2014_Molecules_19_7152

Reference

Title : Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition - Vinsova_2014_Molecules_19_7152
Author(s) : Vinsova J , Kratky M , Komloova M , Dadapeer E , Stepankova S , Vorcakova K , Stolarikova J
Ref : Molecules , 19 :7152 , 2014
Abstract :

A new series of 27 diethyl 2-(phenylcarbamoyl)phenyl phosphorothioates (thiophosphates) was synthesized, characterized by NMR, IR and CHN analyses and evaluated against Mycobacterium tuberculosis H37Rv, Mycobacterium avium and two strains of Mycobacterium kansasii. The best activity against M. tuberculosis was found for O-{4-bromo-2-[(3,4-dichlorophenyl)carbamoyl]phenyl} O,O-diethyl phosphorothioate (minimum inhibitory concentration of 4 microM). The highest activity against nontuberculous mycobacteria was exhibited by O-(5-chloro-2-{[4-(trifluoromethyl)phenyl]carbamoyl}-phenyl) O,O-diethyl phosphorothioate with MIC values from 16 microM. Prepared thiophosphates were also evaluated against acetylcholinesterase from electric eel and butyrylcholinesterase from equine serum. Their inhibitory activity was compared to that of the known cholinesterases inhibitors galanthamine and rivastigmine. All tested compounds showed a higher (for AChE inhibition) and comparable (for BChE inhibition) activity to that of rivastigmine, with IC50s within the 8.04 to 20.2 microM range.

PubMedSearch : Vinsova_2014_Molecules_19_7152
PubMedID: 24886941

Related information

Inhibitor CHEMBL3104293

Citations formats

Vinsova J, Kratky M, Komloova M, Dadapeer E, Stepankova S, Vorcakova K, Stolarikova J (2014)
Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition
Molecules 19 :7152

Vinsova J, Kratky M, Komloova M, Dadapeer E, Stepankova S, Vorcakova K, Stolarikova J (2014)
Molecules 19 :7152