Potential antidepressants: Synthesis of two 4-(aminoalkoxy)dibenzo[b,e]thiepin-11(6H)-ones

1989 ◽  
Vol 54 (1) ◽  
pp. 225-228 ◽  
Author(s):  
Irena Červená ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Jan Metyš ◽  
Martin Valchář ◽  
...  

Heating of 4-methoxydibenzo[b,e]thiepin-11(6H)-one with pyridine hydrochloride to 225 to 235 °C effected demethylation and gave IV. Its sodium salt reacted with 3-dimethylaminopropyl chloride in ethanol and afforded the 4-(3-dimethylaminopropoxy) compound II. The isomeric ether III was prepared via the 4-(4-bromobutoxy) compound V. Hydrochloride of II (VÚFB-17 033) inhibited mildly the binding of [3H]desipramine in rat hypothalamus, had antireserpine activity in rats, mild anticonvulsant effect, and antihypoxic effect in the test of nitrogen anoxia in mice.

2020 ◽  
Vol 8 (38) ◽  
pp. 13368-13374
Author(s):  
Muhammad Umair Khan ◽  
Gul Hassan ◽  
Jinho Bae

This paper proposes a novel soft ionic liquid (IL) electrically functional device that displays resistive memory characteristics using poly(acrylic acid) partial sodium salt (PAA-Na+:H2O) solution gel and sodium hydroxide (NaOH) in a thin polydimethylsiloxane (PDMS) cylindrical microchannel.


2009 ◽  
Vol 22 (2) ◽  
pp. 115-124
Author(s):  
Anna Zadrożniak ◽  
MichaŁ K. Trojnar ◽  
Marcin P. Trojnar ◽  
Żaneta Kimber-Trojnar ◽  
Monika Dudra-Jastrzębska ◽  
...  

2017 ◽  
Vol 70 ◽  
pp. 160-164 ◽  
Author(s):  
G.W. Bourdôt ◽  
S. Jackman ◽  
D.J. Saville

Flupropanate (sodium 2,2,3,3 tetrafluoropropanate), a slow-acting lipid bio- synthesis-inhibiting herbicide, was recently registered in New Zealand as Taskforce (745 g/L flupropanate as the sodium salt) for the selective and long-term control of Nassella trichotoma (nassella tussock) in pastures. In five dose-response experiments in permanent hill pastures in Canterbury, conducted between 2012 and 2016, we measured the efficacy of the herbicide against established plants of N. trichotoma and its residual activity against recruiting seedlings. Mortality, as an average across the five sites, was 93% 1.5 years after applying 1.49 kg flupropanate/ha (the label-recommended rate), and 100% at 2.98 kg/ha. This indicates that an application rate higher than the label rate will be necessary for complete control of a N. trichotoma infestation. The presence of 1,000 and 6,250 visible seedlings of N. trichotoma/ha in the autumn 3.2 and 2.1 years after applying 1.49 kg flupropanate/ha (at a Greta Valley and Scargill site respectively) indicates that the herbicide’s soil residues had decayed within 12 months to a concentration lower than necessary to kill the germinating seedlings of N. trichotoma.


1983 ◽  
Vol 48 (4) ◽  
pp. 1173-1186 ◽  
Author(s):  
Václav Bártl ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Marie Bartošová ◽  
Miroslav Protiva

Reactions of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins XIVa-XIVd with benzaldehyde, 3,4-dimethoxybenzaldehyde, 4-dimethylaminobenzaldehyde, salicylaldehyde, 3-ethoxy-4-hydroxybenzaldehyde, 2-(2-dimethylaminoethoxy)benzaldehyde, 3-(2-dimethylaminoethoxy)benzaldehyde and 3-ethoxy-4-(2-dimethylaminoethoxy)benzaldehyde afforded a series of 19 hydrazones IIIa-Xc. Some of them showed the expected anticonvulsant effect but only towards pentetrazole; antagonism of maximal electroshock seizures was not observed. In general, the products have a character of tranquillizers: in higher does they produce central depression, potentiate the thiopental sleeping time, have hypothermic action; in single cases antiamphetamine, antireserpine, antihistamine and cataleptic effects were observed. The water-soluble salts of the basic hydrazones VIIIa, VIIIc, IXc and Xc, administered parenterally, showed a rather high acute toxicity and revealed also adrenolytic and hypotensive activity.


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