scholarly journals Cu(OAc)2 as a green promoter for one-pot synthesis of 2-amino-4,6-diarylpyridine- 3-carbonitrile as antibacterial agents

2020 ◽  
Vol 34 (1) ◽  
pp. 149-156
Author(s):  
Bi Bi Fatemeh Mirjalili ◽  
Soghra Khabnadideh ◽  
Ahmad Gholami ◽  
Leila Zamani ◽  
Leila Zamani ◽  
...  

The extensive use of antimicrobial drugs and their resistance against bacterial infections have led to discover new antimicrobial compounds. In this study, we wish to report, one-pot synthesis of 2-amino-3-cyanopyridine derivatives (1a-14a). These compounds were synthesized in the presence of Cu(OAc)2 as a highly effective heterogeneous acid catalyst. Here we evaluated the antimicrobial activities of these compounds against different species of microorganisms including gram positive and gram negative bacteria as well as fungi. Standard antimicrobial methods include disc diffusion and Broth microdilution method according to the protocol of the Clinical and Laboratory Standards Institute (CLSI). Synthesis of 2-amino-3-cyanopyridine derivatives were done via reaction of aromatic aldehydes, acetophenone derivatives, malononitrile and ammonium acetate in the presence of Cu(OAc)2 under reflux condition. The results show compound 2-amino-6-(4-chlorophenyl)-4-phenylnicotinonitrile (10a) had the best antimicrobial efficacy toward C. albicans, E. faecalis, P. aeroginosa and E. coli. In conclusion, comparing the structure and activity of the compounds (10a), this compound with the presence of Cl residue at para-position of phenyl ring improves the antibacterial and antifungal activity.   Bull. Chem. Soc. Ethiop. 2020, 34(1), 149-156. DOI: https://dx.doi.org/10.4314/bcse.v34i1.14

2017 ◽  
Vol 43 (3) ◽  
pp. 220-227
Author(s):  
Gülhan Turan-Zitouni ◽  
Betül Kaya Çavuşoğlu ◽  
Begüm Nurpelin Sağlık ◽  
Ulviye Acar Çevik

Abstract Objective: The advent of resistant pathogenic microorganisms against current antimicrobial drugs prompted scientists to investigate novel molecules with new mechanisms. In this paper, some new 2-[2-[4-(ethyl/phenyl)cyclohexylidene]hydrazinyl]-4-(4-substitutedphenyl)thiazole (2a–2o) derivatives were synthesized and studied for their antimicrobial activities. Materials and methods: The title compounds (2a–2o) were obtained via the reaction of 4-(ethyl/phenyl)cyclohexane-1-one with appropriate phenacyl bromide in ethanol at room temperature. The chemical structures of the compounds were elucidated by FT-IR, 1H-NMR, 13C-NMR, HRMS and elemental analysis. Antimicrobial activity of the compounds was measured by using broth microdilution method. Chloramphenicol and ketoconazole were used as reference drugs. Results: Among the synthesized compounds, 2-[2-(4-phenylcyclohexylidene)hydrazinyl]-4-phenylthiazole (2h) and 2-[2-(4-phenylcyclohexylidene)hydrazinyl]-4-(4-chlorophenyl)thiazole (2l) have been found to exhibit potency almost four-fold better than ketoconazole against C. albicans with MIC90 value of 1.95. Conclusion: The current study contributed to the knowledge of the antimicrobial activity of thiazole bearing compounds.


2017 ◽  
Vol 58 (2) ◽  
Author(s):  
Ghodsi Mohammadi Ziarani ◽  
Somayeh Mousavi ◽  
Mahshid Rahimifard ◽  
Alireza Badiei

One-pot synthesis of benzo[<em>c</em>]acridine derivatives via the three-component condensation reaction of aromatic aldehydes, 1-naphtylamine, and dimedone using sulfonic acid functionalized SBA-15 (SBA-Pr-SO<sub>3</sub>H) as nanoporous acid catalyst under solvent-free conditions was studied. This reaction is an efficient, green and  environmentally friendly procedure.


RSC Advances ◽  
2015 ◽  
Vol 5 (61) ◽  
pp. 49295-49300 ◽  
Author(s):  
Handan Pamuk ◽  
Burak Aday ◽  
Fatih Şen ◽  
Muharrem Kaya

Pt NPs@GO has been used for the first time for synthesizing acridinedione from dimedone, aromatic aldehydes and various amines as a catalyst.


2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Johana Rondevaldova ◽  
Olga Leuner ◽  
Alemtshay Teka ◽  
Ermias Lulekal ◽  
Jaroslav Havlik ◽  
...  

Bacterial infections are in less-developed countries traditionally treated by remedies prepared from medicinal plants.Embelia schimperi(Vatke) is a plant used as a taenicide or disinfectant in Ethiopia, very often taken mixed with another plant species. In the present study, we examined two extracts prepared from seeds and twigs with leaves ofE. schimperiand its main present secondary metabolite embelin for their antibacterial combinatory effect with oxacillin and tetracycline against sensitive and resistantStaphylococcus aureusstrains. Minimum inhibitory concentrations were determined through the broth microdilution method, whereas the combinatory effect was evaluated through fractional inhibitory concentration sum (ΣFIC) indices. Results show many positive interactions and synergy occurring in embelin and oxacillin combinations against 4 out of 9 strains (ΣFIC 0.203–0.477) and for embelin and tetracycline combination against 3 out of 9 strains (ΣFIC 0.400–0.496). Moreover, the resistance to oxacillin has been overcome in 2 strains and to tetracycline in 3 strains. According to our knowledge, this is the first study showing antimicrobial combinatory effect ofE. schimperias well as of embelin. These findings can be used for the further research targeted on the development of new antistaphylococcal agents.


2021 ◽  
pp. 132260
Author(s):  
Y. Narasimha Reddy ◽  
Radhakrishna Reddy Mardi ◽  
Nagaraja Reddy G ◽  
Sreenivasulu Reddy T ◽  
Kondaiah Seku ◽  
...  

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