Potential antidepressants. Synthesis of 6,11-dihydrodibenzo[b,e]thiepin-11-yl (dimethylaminomethyl)phenyl ethers, sulfides, amines and some related compounds

1990 ◽  
Vol 55 (1) ◽  
pp. 282-295 ◽  
Author(s):  
Karel Šindelář ◽  
Vladimír Valenta ◽  
Jiří Holubek ◽  
Oluše Matoušová ◽  
Miroslav Protiva

Reactions of 11-chloro-6,11-dihydrodibenzo[b,e]thiepin and its 2-bromo derivative with the isomeric (dimethylaminomethyl)phenols, (dimethylaminomethyl)thiophenols, and (dimethylaminomethyl)anilines in toluene afforded the title compounds IIIb,c, Va, VIIIa,b,c, and Xa,b,c. Reactions of 11-chloro-6,11-dihydrodibenzo[b,e]thiepin and its 2-chloro and 2-methyl derivatives with N,N-dimethyl-2-(4-aminophenoxy)ethylamine and N,N-dimethyl-3-(4-aminophenoxy)propylamine by heating in dimethylformamide in the presence of sodium carbonate gave the diamino ethers XI-XIV. The compounds showed only indications of the antidepressant agents profile and some antimicrobial effects in vitro.

2021 ◽  
Vol 27 ◽  
pp. 102369
Author(s):  
Shijun Lu ◽  
Xiaochen Tang ◽  
Qingqing Lu ◽  
Jiwei Huang ◽  
Xinran You ◽  
...  

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 708
Author(s):  
Radek Sleha ◽  
Vera Radochova ◽  
Jiri Malis ◽  
Alexander Mikyska ◽  
Milan Houska ◽  
...  

Staphylococcus (S.) aureus is an important causative agent of wound infections with increasing incidence in the past decades. Specifically, the emergence of methicillin-resistant S. aureus (MRSA) causes serious problems, especially in nosocomial infections. Therefore, there is an urgent need to develop of alternative or supportive antimicrobial therapeutic modalities to meet these challenges. Purified compounds from hops have previously shown promising antimicrobial effects against MRSA isolates in vitro. In this study, purified beta-acids from hops were tested for their potential antimicrobial and healing properties using a porcine model of wounds infected by MRSA. The results show highly significant antimicrobial effects of the active substance in both the powder and Ambiderman-based application forms compared to both no-treatment control and treatment with Framycoin. Moreover, the macroscopic evaluation of the wounds during the treatment using the standardized Wound Healing Continuum indicated positive effects of the beta-acids on the overall wound healing. This is further supported by the microscopic data, which showed a clear improvement of the inflammatory parameters in the wounds treated by beta-acids. Thus, using the porcine model, we demonstrate significant therapeutic effects of hops compounds in the management of wounds infected by MRSA. Beta-acids from hops, therefore, represent a suitable candidate for the treatment of non-responsive nosocomial tissue infections by MRSA.


2021 ◽  
Author(s):  
M. Beukema ◽  
K. Ishisono ◽  
J. de Waard ◽  
M. M. Faas ◽  
P. de Vos ◽  
...  

Pectins inhibit the growth of C. rodentium in vitro, preventing attachment of C. rodentium to CMT93 epithelial cells. Through these antimicrobial effects, pectins protect the epithelium from C. rodentium-induced barrier dysfunction and damage.


1980 ◽  
Vol 32 (1) ◽  
pp. 751-756
Author(s):  
HILARY J. LITTLE ◽  
J. M. H. REES
Keyword(s):  

Author(s):  
TITTY SULIANTI ◽  
NILAKESUMA DJAUHARI ◽  
BAMBANG NURSASONGKO

Objective: The aim is to compare the antimicrobial effects of papain and Papacarie with dilution and diffusion tests.Methods: There were two treatment groups and one Group control. The treatment group received papain and Papacarie, and the control groupreceived chlorhexidine, in five liquids with different concentrations of 0.5%, 0.25%, 0.125%, 0.0625%, and 0.03%. The dilution and diffusion testswere used to determine the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and zone of inhibition for eachtreatment material.Results: MICs of papain and Papacarie were 12.5%, indicating that at a concentration of 12.5%, the material can inhibit the growth of Streptococcusmutans. Papain does not have an MBC value but the Papacarie has an MBC at 25%, which indicating that at a concentration of 25%, Papacarie hasbactericidal effects on S. mutans. The zone of inhibition of papain was lower than Papacarie.Conclusion: Based on chemomechanical caries removal materials, the antimicrobial effects of Papacarie were better than those of papain.


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