Synthesis and in vitro evaluation of 2-(((2-ether)amino)methylene)-dimedone derivatives as potential antimicrobial agents

Lone, Ali Mohd; Rather, Muzafar Ahmad; Bhat, Muneer Ahmad; Bhat, Zubair Shanib; Tantry, Irfan Qadir; Prakash, Poonam

doi:10.1016/j.micpath.2017.12.022

Cited by 16 publications

(3 citation statements)

References 18 publications

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“…As supporting information for the Malaria Box, plate mapping and complete data with the original GSK/St Jude/Novartis compound number, ID, set, molecular weight, canonical SMILES, source, and biological data are provided as supporting information for Malaria Box [26][27][28]. Additionally available [28][29][30] is a list of vendors that provided the compounds for the Malaria Box, along with the number of compounds from each vendor and their website address.…”

Section: Chemical Reagentsmentioning

confidence: 99%

“…For the preparation of bacterial inoculum, 1 mL of 24 h culture was suspended in 9 mL of sterile broth. The bacterial suspension was further diluted through five-fold broth dilution, and the last one was used in the experiment, with 25 µL added to each well of the micro-titer plate and prepared freshly every time [30]. A total of 25 µL of the liquid drug and 25 µL of the sterile broth were added and mixed in the first well, which contained the highest concentration of drug.…”

Section: Microdilution Assays and Minimum Inhibitory Concentration (Mic)mentioning

confidence: 99%

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In Vitro Activity and Atom Pair Fingerprint Analysis of Potent Hits from Malaria Box against Staphylococcus aureus Isolated from Cows with Clinical Mastitis

Mansour,

Elkenany,

Awad

et al. 2023

Dairy

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Staphylococcus aureus (S. aureus) is one of the most prevalent contagious bacterial pathogens causing clinical bovine mastitis. In the present study, plate (A), which consists of 80 compounds (40 drug-like and 40 probe-like), was assessed from the Malaria Box against the in vitro growth of S. aureus isolated from cows naturally infected with S. aureus. Anti-Staphylococcus aureus medications that are newer and more potent than those that have been used previously were discovered. Bioinformatics analysis for the potent identified hits was performed. Three compounds—two probe-like and one drug-like—showed strong inhibitory action against S. aureus growth in vitro. Among these hits, MMV665941 exhibited the highest minimum inhibitory concentration value of 0.0078. Combination therapy was carried out using the most potent anti-S. aureus medication, MMV665941, and the traditionally used anti-S. aureus drug, amoxicillin/clavulanate (Augmentin 625®). The atom pair fingerprint (APfp) analysis revealed that MMV665941 and Augmentin showed maximum structural similarity. Based on the results obtained, it can be concluded that the Medicines for Malaria Venture Box has a wealth of potential anti-S. aureus candidates.

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Section: Chemical Reagentsmentioning

confidence: 99%

Section: Microdilution Assays and Minimum Inhibitory Concentration (Mic)mentioning

confidence: 99%

In Vitro Activity and Atom Pair Fingerprint Analysis of Potent Hits from Malaria Box against Staphylococcus aureus Isolated from Cows with Clinical Mastitis

Mansour,

Elkenany,

Awad

et al. 2023

Dairy

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“…It is used in the synthesis of selective heterocyclic moieties that are industrial as well as pharmacologically important [5][6][7][8][9][10][11]. Dimedone and its analogs own many therapeutic properties such as antioxidant [12,13], anticarcinogenic [14], anticoagulant [15], antihistaminic [16], and antimicrobial [17]. The cited properties of dimedone along with its huge accessibility and easy handling, low toxicity, cost-efficiency, and moisture stability has developed unusual interests in organic chemists.…”

Section: Introductionmentioning

confidence: 99%

Advancement in synthetic strategies of bisdimedones: Two decades study

Teli¹,

Sahiba²,

Sethiya³

et al. 2021

Journal of Heterocyclic Chem

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Bisdimedones have emerged as an important and versatile moiety in the field of synthetic and medicinal chemistry. It is screened as a precursor for the synthesis of several heterocycles such as acridinediones, xanthenediones, thioxanthenes, and benzopyrans that exhibited immense pharmacological as well as industrial applications. Its extensive characteristics have attracted the scientists to develop various protocols for the synthesis of bisdimedones and their derivatives from the reaction of dimedone with several aldehydes under different environmental conditions using various types of catalysts. This review encapsulates the recent progress in the synthesis of bisdimedone derivatives under several reaction protocols such as the use of nanoparticles, ionic liquids, metal salts, simple organic compounds, and catalyst-free conditions, and so forth in the last 20 years.

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