Synthesis and Antimicrobial Studies of Coumarin-Substituted Pyrazole Derivatives as Potent Anti-Staphylococcus aureus Agents

Abstract

In this paper, synthesis and antimicrobial studies of 31 novel coumarin-substituted pyrazole derivatives are reported. Some of these compounds have shown potent activity against methicillin-resistant Staphylococcus aureus (MRSA) with minimum inhibitory concentration (MIC) as low as 3.125 µg/mL. These molecules are equally potent at inhibiting the development of MRSA biofilm and the destruction of preformed biofilm. These results are very significant as MRSA strains have emerged as one of the most menacing pathogens of humans and this bacterium is bypassing HIV in terms of fatality rate.

Synthesis of 4,4′-(4-Formyl-1H-pyrazole-1,3-diyl)dibenzoic Acid Derivatives as Narrow Spectrum Antibiotics for the Potential Treatment of Acinetobacter Baumannii Infections

“…Fluoro-substitution on the phenyl ring increased the potency of molecules significantly [ 16 , 17 ]. Similarly, coumarin and naphthalene substituted compounds also showed potent activity against the tested strains, particularly S. aureus [ 18 , 19 , 20 ]. Our reported molecules are significantly lipophilic.…”

Trending Topics on Coumarin and Its Derivatives in 2020

“…There are several works in which antibacterial activity is found due to the presence of an azole ring introduced in different positions of the coumarin system. Articles have been published recently on the antibacterial activity of azole–coumarins, as well as 3/4/7 substituted arylcoumarins ( Figure 3 , general structures VII and VIII ), especially active on Gram-positive and negative bacteria according to substitution patterns [ 15 , 18 , 19 , 20 ]. In other cases, thiazolidinedione–coumarin hybrids have been described ( Figure 3 , general structure IX ) that show activity on methicillin-resistant Staphylococcus aureus (MRSA) [ 21 ].…”

1,2,4-Oxadiazole-Based Bio-Isosteres of Benzamides: Synthesis, Biological Activity and Toxicity to Zebrafish Embryo

“…However, as people’s environmental awareness gradually deepens, high-efficiency, low-toxicity, and environmentally friendly pesticides have become an inevitable trend in the creation of new pesticides [ 1 , 2 , 3 ]. There is no doubt that heterocyclic structures are important feature in synthetic pesticides for their high-efficiency, various biological activities, and diversity of possible substituents [ 4 , 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 ]. 1,2,4-Oxadiazole heterocycle, as an important kind of the five-membered oxygen-nitrogen heterocycle, has exhibited a wide range of biological activities in the field of pesticides, such as insecticidal [ 26 , 27 , 28 ], antifungal [ 29 , 30 ], and herbicidal activities [ 31 ].…”