ChemInform Abstract: NEW MANNICH BASES FROM 5-(METHYLPHENOXYMETHYL)-1,3,4-OXADIAZOLE-2-THIONE DERIVATIVES AND THEIR BACTERICIDAL PROPERTIES

1978 ◽  
Vol 9 (45) ◽  
Author(s):  
A. K. SENGUPTA ◽  
O. P. BAJAJ
2019 ◽  
Vol 0 (2) ◽  
pp. 21-25
Author(s):  
M.A. Guseinova ◽  
◽  
E.V. Salomatina ◽  
L.A. Smirnova ◽  
O.N. Smirnova ◽  
...  

Author(s):  
Serhii Zinoviev ◽  
Andrii Kurman ◽  
Dmytro Bindiug ◽  
Pavlo Grubich ◽  
Liubov Lepeta

The introduction of the newest technologies of organic pig breeding has the basic principle of minimizing the use in pigs of chemicals, trace amounts of which in pig production adversely affect the quality of products and the health of consumers. The transition to herbal remedies, the maximum possible rejection of chemical synthesis products, is inhibited, in the main, by the relatively small spectrum of plant compounds with the investigated activity. According to the results of previous studies, six working solutions of Juglans regia L phytosupply extracts - potential phytosine disinfectants were developed: To investigate the bactericidal activity of the experimental preparations of Juglans regia, flushes were made from the internal structures and technological equipment of the housing of the pig stock of the experimental base v. Takhtaulove. Obtained samples of typical banal microflora of the pig complex were mixed to obtain a bacterial-containing suspension averaged over the concentration of microbial bodies and the spectrum of types of microflora in the microbiota. When cultured on nutrient media, with the superficial sowing of a suspension of banal microflora of a pig in the presence of a potential phytodisinfectant, processes of development of individual colonies of the microflora are observed. The amount and intensity of their development, the degree of inhibition of life, assess the level of bactericidal activity of the extracts. The highest bactericidal and fungicidal activity, and consequently, the potential efficacy as a possible disinfectant in the technology of organic pig breeding was revealed by the extracts of phytosupply Juglans regia L No. 2 (extractant - acetic acid to 5 %, nut of wax ripeness) and 4 (extractant, alcohol 20 % nutrient wax ripeness (proven after obtaining the primary extract of up to 5 % alcohol), which have bactericidal properties against gram-positive cocci and gram-negative sticks, but have a weak effect on the spore-forming bacilli. Key words: organic pig breeding, bactericidal activity, phyto-disinfectant, commonplace typical microflora of a pig complex, phyto row materials, walnut extract.


2016 ◽  
Vol 4 (11) ◽  
pp. 892-899
Author(s):  
AbdelKarim M. ◽  
◽  
Wafa O. ◽  
Nafesa A.G. ◽  
Inas O. ◽  
...  

2016 ◽  
Vol 13 (8) ◽  
pp. 734-741 ◽  
Author(s):  
Kaan Kucukoglu ◽  
Halise Inci Gul ◽  
Mustafa Gul ◽  
Rengul Cetin-Atalay ◽  
Yosra Baratli ◽  
...  

2020 ◽  
Vol 17 (4) ◽  
pp. 512-517
Author(s):  
Ognyan Ivanov Petrov ◽  
Yordanka Borisova Ivanova ◽  
Mariana Stefanova Gerova ◽  
Georgi Tsvetanov Momekov

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.


2020 ◽  
Vol 16 (4) ◽  
pp. 531-543
Author(s):  
Shaheen Faizi ◽  
Tahira Sarfaraz ◽  
Saima Sumbul ◽  
Almas Jabeen ◽  
Sobia A. Halim ◽  
...  

Background: In continuation of our work on Mannich reaction on 8-hydroxyquinoline, fifteen different combinations of aromatic aldehydes and aniline were subjected to Mannich reaction from which twelve products (eight Mannich bases, two imines and two intramolecularly cyclized products with benzofuranone skeleton) were obtained. Among them six compounds (1, 2, 6, 8, 9 and 12) are the new compounds. The structures of the compounds were characterized by UV, IR, MS and 1H NMR. Method: The compounds were tested for the inhibition of pro-inflammatory cytokines tumor necrosis factor-α (TNF-α) and Interleukin-1β (IL-1β) at a concentration of 25 µg/mL. The cytokines were produced by THP-1 cells differentiated with PMA for 24hrs and stimulated with LPS for 4 hrs and supernatant were analyzed through ELISA technique. Results and Discussion: Compounds 1-5, 8 and 9 inhibited the production of TNF-α and IL-1β. Compounds 1, 3, and 8 exerted potent inhibitions of TNF-α with 71%, 71%, and 83% inhibition, respectively. Compounds 1 and 8 significantly inhibited the production of IL-1β with 64% and 78% inhibition, respectively. Conclusion: Compounds 1 and 8 significantly inhibited the production of IL-1β with 64% and 78% inhibition, respectively. Notably compound 8 showed the most potent inhibition of these cytokines. Additionally, the effect of compounds on viability of THP-1 cells was also evaluated. Moreover, molecular docking was carried out to study the mechanism of inhibition of TNF-α production.


2013 ◽  
Vol 9 (3) ◽  
pp. 379-383 ◽  
Author(s):  
Susanta Roy ◽  
Dipak Chetia ◽  
Mithun Rudrapal ◽  
Anil Prakash

2019 ◽  
Vol 57 (1) ◽  
pp. 346-354
Author(s):  
Elsayed M. Afsah ◽  
Ez‐el‐Din M. Kandil ◽  
Soha M. Abdelmageed ◽  
Fatma T. Elbarhmtoushi
Keyword(s):  

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