Abstract
A series of 1ʹ-acetoxychavicol acetate analogues were synthesised and evaluated for their antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) using broth microdilution technique. The minimum inhibitory concentration (MIC) was used to determine whether the compounds had potential as inhibitory agents against the MRSA ATCC 43300, and the compounds with antimicrobial potential (<2000 μg ml–1) were tested for minimum bactericidal concentration (MBC). Based on this assay, compound 1 exhibited potent antimicrobial activity with MIC value of 250 μg ml–1. Meanwhile, compounds 2 and 13 showed the moderate activity with MIC values of 500 μg ml–1, respectively.
Highlights
The infectious diseases caused by antibiotic resistance pathogens have been increasing significantly over the last few decades due to the widespread use of antibiotics
In Malaysia, the prevalence of Methicillin-resistant Staphylococcus aureus (MRSA) infections increased from 18.0% in 2016 to 19.8% in 2017, and it is listed as one of the seven pathogens associated with high mortality.[3,4]
We describe the synthesis and antimicrobial evaluation of ACA analogues against MRSA (Figure 1)
Summary
The infectious diseases caused by antibiotic resistance pathogens have been increasing significantly over the last few decades due to the widespread use of antibiotics. Treatments for MRSA infection are limited because MRSA strains are often resistant towards first-line beta-lactam antibiotics such as methicillin, oxacillin, penicillin and amoxycilin.[5] Since the antibiotic resistance has reached an alarming level, there is great need to develop new antibacterials.[6] In the search for new antimicrobial compounds, medicinal plants are valuable sources of potent drugs due to the presence of a variety of active chemical substances.[7] An example of such a plant is Alpinia conchigera Griff., locally known as cengkenam, lengkuas kecil, lengkuas padang, lengkuas ranting or lengkuas genting.[8] This species belongs to the Zingiberaceae family, and the rhizomes of this species is commonly used as spice or ginger substitutes for flavouring food.[8] In Peninsular Malaysia, the young shoots of rhizomes are often used in vegetarian dishes, post-partum treatment and treatment of fungal infections as part of traditional medicine.[9] There have been a few studies on the chemical constituents from rhizome of Alpinia conchigera. The structural activity relationship of ACA were observed by comparing the inhibition activities with structural features of analogues
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