scholarly journals 2-(chromon-3-yl)imidazole derivatives as potential antimicrobial agents: synthesis, biological evaluation and molecular docking studies

2016 ◽  
Vol 10 (1) ◽  
pp. 35-44 ◽  
Author(s):  
Shweta Sharma ◽  
Vishal Sharma ◽  
Gurpreet Singh ◽  
Harpreet Kaur ◽  
Shubham Srivastava ◽  
...  
2019 ◽  
Vol 194 (9) ◽  
pp. 887-894 ◽  
Author(s):  
Firuze Diyar Altındağ ◽  
Begüm Nurpelin Sağlık ◽  
Ulviye Acar Çevik ◽  
İlhan Işıkdağ ◽  
Yusuf Özkay ◽  
...  

Antibiotics ◽  
2019 ◽  
Vol 8 (4) ◽  
pp. 178 ◽  
Author(s):  
Mahadev Patil ◽  
Anurag Noonikara-Poyil ◽  
Shrinivas D. Joshi ◽  
Shivaputra A. Patil ◽  
Siddappa A. Patil ◽  
...  

A series of new urea derivatives, containing aryl moieties as potential antimicrobial agents, were designed, synthesized, and characterized by 1H NMR, 13C NMR, FT-IR, and LCMS spectral techniques. All newly synthesized compounds were screened in vitro against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). Variable levels of interaction were observed for these urea derivatives. However, and of major importance, many of these molecules exhibited promising growth inhibition against Acinetobacter baumannii. In particular, to our delight, the adamantyl urea adduct 3l demonstrated outstanding growth inhibition (94.5%) towards Acinetobacter baumannii. In light of this discovery, molecular docking studies were performed in order to elucidate the binding interaction mechanisms of the most active compounds, as reported herein.


2020 ◽  
Vol 30 (17) ◽  
pp. 127368
Author(s):  
Eugenia Stingaci ◽  
Marina Zveaghinteva ◽  
Serghei Pogrebnoi ◽  
Lucian Lupascu ◽  
Vladimir Valica ◽  
...  

Antibiotics ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 309
Author(s):  
Michelyne Haroun ◽  
Christophe Tratrat ◽  
Aggeliki Kolokotroni ◽  
Anthi Petrou ◽  
Athina Geronikaki ◽  
...  

In this study, we report the design, synthesis, computational and experimental evaluation of the antimicrobial activity, as well as docking studies of new 5-methylthiazole based thiazolidinones. All compounds demonstrated antibacterial efficacy, some of which (1,4,10 and 13) exhibited good activity against E. coli and B. cereus. The evaluation of antibacterial activity against three resistant strains, MRSA, P. aeruginosa and E. coli, revealed that compound 12 showed the best activity, higher than reference drugs ampicillin and streptomycin, which were inactive or exhibited only bacteriostatic activity against MRSA, respectively. Ten out of fifteen compounds demonstrated higher potency than reference drugs against a resistant strain of E. coli, which appeared to be the most sensitive species to our compounds. Compounds 8, 13 and 14 applied in a concentration equal to MIC reduced P. aeruginosa biofilm formation by more than 50%. All compounds displayed antifungal activity, with compound 10 being the most active. The majority of compounds showed better activity than ketoconazole against almost all fungal strains. In order to elucidate the mechanism of antibacterial and antifungal activities, molecular docking studies on E. coli Mur B and C. albicans CYP51 and dihydrofolate reductase were performed. Docking analysis of E. coli MurB indicated a probable involvement of MurB inhibition in the antibacterial mechanism of tested compounds while docking to 14α-lanosterol demethylase (CYP51) and tetrahydrofolate reductase of Candida albicans suggested that probable involvement of inhibition of CYP51 reductase in the antifungal activity of the compounds. Potential toxicity toward human cells is also reported.


Sign in / Sign up

Export Citation Format

Share Document