ChemInform Abstract: Synthesis and Structure Elucidation of Some New Thioether Derivatives of 1,2,4-Triazoline-3-thiones and Their Antimicrobial Activities.

ChemInform ◽  
2010 ◽  
Vol 33 (17) ◽  
pp. no-no
Author(s):  
N. N. Guelerman ◽  
H. N. Dogan ◽  
S. Rollas ◽  
C. Johansson ◽  
C. Celik
Il Farmaco ◽  
2001 ◽  
Vol 56 (12) ◽  
pp. 953-958 ◽  
Author(s):  
N.N Gülerman ◽  
H.N Doğan ◽  
S Rollas ◽  
C Johansson ◽  
C Çelik

2020 ◽  
Vol 17 ◽  
Author(s):  
Rahele Bargebid ◽  
Ali Khalafi-Nezhad ◽  
Kamiar Zomorodian ◽  
Leila Zamani ◽  
Ali Ahmadinejad ◽  
...  

Introduction: Mannich reaction is a typical example of a three-component condensation reaction and the chemistry of Mannich bases has been the matter of search by researchers. Here an efficient procedure for the synthesis of some new Mannich derivatives of simple phenols is described. Methods: In this procedure a microwave-assisted and solvent less condensation were done between different phenols, secondary amines and paraformaldehyde. The reactions proceed in the presence of catalytic amount of nano ZnO and tetrabutylammonium bromide (TBAB) in excellent yields. 10 new compounds were synthesized (A1-A10). Chemical structures of all new compounds were confirmed by different spectroscopic methods. We optimized the chemical reactions in different conditions. Optimization reactions were done in the presence of different mineral oxides, different amount of TBAB and also different solvents. Nano ZnO and TBAB in catalytic amounts and solvent free conditions were the best conditions. All the synthesized compounds were screened for their antimicrobial activities. Antifungal and antibacterial activities of the synthesized compounds were evaluated against some Candida, filaments fungi, gram positive and gram negative bacteria by broth micro dilution method as recommended by CLSI. Results: The result showed that compounds A2, A3 and A4 against most of the tested Candida species and compounds A5 and A7 against C. parapsilosis and C. tropicalis, exhibited considerable antifungal activities. Also Compounds A8 and A10 showed desirable antifungal activities against C. neoformance and C. parapsilosis, respectively. The antibacterial activities of the synthesized compounds were also evaluated. Compounds A6 - A10 against E. Fecalis and compounds A5, A7, A9 and A10 against P. aeruginosa showed desirable antibacterial activities. Discussion: We have synthesized some new Mannich adducts of poly-hydroxyl phenols in the presence of nano-ZnO as a reusable catalyst, with the hope of discovering new lead compounds serving as potent antimicrobial agents. The advantages of this method are generality, high yields with short reaction times, simplicity, low cost and matching with green chemistry protocols. The antimicriobial studies of Mannich derivatives of phenols showed desirable results in vitro.


Marine Drugs ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 35
Author(s):  
Mohamed Shaaban ◽  
Ghada S. E. Abou-El-Wafa ◽  
Christopher Golz ◽  
Hartmut Laatsch

Analysis of the air-dried marine red alga Laurencia papillosa, collected near Ras-Bakr at the Suez gulf (Red Sea) in Egypt delivered five new halogenated terpene derivatives: aplysiolic acid (1), 7-acetyl-aplysiol (2), aplysiol-7-one (3), 11,14-dihydroaplysia-5,11,14,15-tetrol (5a), and a new maneonene derivative 6, named 5-epi-maneolactone. The chemical structures of these metabolites were characterized employing spectroscopic methods, and the relative and absolute configurations were determined by comparison of experimental and ab initio-calculated NMR, NOE, ECD, and ORD data, and by X-ray diffraction of 2 and 6. The antimicrobial activities of the crude extract and compounds 1–3, 5a and 6 were studied.


2013 ◽  
Vol 8 (1) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Ismail Kiran ◽  
Özge Özşen ◽  
Turgay Çelik ◽  
Semra İlhan ◽  
Bükay Yenice Gürsu ◽  
...  

Isophorone (3,5,5-trimethyl-2-cyclohexen-1-one), a monoterpene, and the structurally related 1,8-cineole and camphor, have demonstrated a protective effect against cancer, biological activity against a variety of microorganisms, and anti-oxidant properties. The derivatization of isophorone is, therefore, an important field of xenobiochemistry, pharmacology and toxicology. The aim of this study was to obtain derivatives of isophorone through microbial biotransformation and evaluate the biotransformation metabolites as potential antimicrobial agents. Incubation of isophorone with the fungi Alternaria alternata and Neurospora crassa afforded 4α-hydroxy- and 7-hydroxy-isophorone as transformation metabolites. The antimicrobial activities of isophorone and the metabolites were evaluated in vitro both by using agar dilution and microdilution methods. However, no significant antibacterial activity was observed when compared with those of standard substances.


2017 ◽  
Vol 53 (1) ◽  
pp. 109-113 ◽  
Author(s):  
Xue-Qing Zhang ◽  
Fei-Fei Guan ◽  
De-Bao Li ◽  
Chang-Yun Wang ◽  
Chang-Lun Shao

Molecules ◽  
2020 ◽  
Vol 25 (16) ◽  
pp. 3577
Author(s):  
Yuri E. Sabutski ◽  
Ekaterina S. Menchinskaya ◽  
Ludmila S. Shevchenko ◽  
Ekaterina A. Chingizova ◽  
Artur R. Chingizov ◽  
...  

A series of new tetracyclic oxathiine-fused quinone-thioglycoside conjugates based on biologically active 1,4-naphthoquinones and 1-mercapto derivatives of per-O-acetyl d-glucose, d-galactose, d-xylose, and l-arabinose have been synthesized, characterized, and evaluated for their cytotoxic and antimicrobial activities. Six tetracyclic conjugates bearing a hydroxyl group in naphthoquinone core showed high cytotoxic activity with EC50 values in the range of 0.3 to 0.9 μM for various types of cancer and normal cells and no hemolytic activity up to 25 μM. The antimicrobial activity of conjugates was screened against Gram-positive bacteria (Staphylococcus aureus, Bacillus cereus), Gram-negative bacteria (Pseudomonas aeruginosa and Escherichia coli), and fungus Candida albicans by the agar diffusion method. The most effective juglone conjugates with d-xylose or l-arabinose moiety and hydroxyl group at C-7 position of naphthoquinone core at concentration 10 µg/well showed antimicrobial activity comparable with antibiotics vancomicin and gentamicin against Gram-positive bacteria strains. In liquid media, juglone-arabinosidic tetracycles showed highest activity with MIC 6.25 µM. Thus, a positive effect of heterocyclization with mercaptosugars on cytotoxic and antimicrobial activity for group of 1,4-naphthoquinones was shown.


2010 ◽  
Vol 7 (2) ◽  
pp. 496-500 ◽  
Author(s):  
Ravindra Kumar ◽  
Y. K. Srivastava

3, 5-Diaryl-2-pyrazoline-1-carbaldehyde(1)was condensed with hydrazine hydrate ando-phenylene diamine to afford corresponding hydrazones(2)and 3-benzimidazolyl-3, 5-diaryl-2-pyrazoline respectively under MWI condition. The newly synthesized compounds have been screened for their antibacterial activityin vitro.


2009 ◽  
Vol 6 (4) ◽  
pp. 1205-1210 ◽  
Author(s):  
J. J. Vora ◽  
S. B. Vasava ◽  
K. C. Parmar ◽  
S. K. Chauhan ◽  
S. S. Sharma

Schiff base derivatives ofN-{(1E)-[3-(mono or di-substituted aryl)-1-phenyl-1H-pyrazol-4-yl]methylene{-4-methylpyridin-2-amine were synthesized by the acid catalyzed condensation of 3-(mono- or di- substituted aryl)-1-phenyl-1H-pyrazole-4-carbaldehyde derivatives with 4-methylpyridin-2-amine. Schiff base derivatives were characterized by FT-IR,1H-NMR, Mass spectral analysis and elemental analysis. All the synthesized compounds have been screened for their antimicrobial activities by using broth dilution method.


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