Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F14%3A39897931" target="_blank" >RIV/00216275:25310/14:39897931 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00216208:11160/14:10281975

Výsledek na webu

<a href="http://dx.doi.org/10.3390/molecules19067152" target="_blank" >http://dx.doi.org/10.3390/molecules19067152</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/molecules19067152" target="_blank" >10.3390/molecules19067152</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition

Popis výsledku v původním jazyce

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 H(37)Rv, 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 mu M). The highest activity against nontuberculous mycobacteriawas exhibited by O-(5-chloro-2-{[4-(trifluoromethyl) phenyl] carbamoyl}phenyl) O, O-diethyl phosphorothioate with MIC values from 16 mu M. 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) ac

Název v anglickém jazyce

Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition

Popis výsledku anglicky

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 H(37)Rv, 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 mu M). The highest activity against nontuberculous mycobacteriawas exhibited by O-(5-chloro-2-{[4-(trifluoromethyl) phenyl] carbamoyl}phenyl) O, O-diethyl phosphorothioate with MIC values from 16 mu M. 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) ac

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CE - Biochemie

OECD FORD obor

—

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2014

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Molecules

ISSN

1420-3049

e-ISSN

—

Svazek periodika

19

Číslo periodika v rámci svazku

6

Stát vydavatele periodika

CH - Švýcarská konfederace

Počet stran výsledku

17

Strana od-do

7152-7168

Kód UT WoS článku

000338586700015

EID výsledku v databázi Scopus

—