Abstract
Development of multidrug resistance (MDR) to antimicrobial, antiparasitic and chemotherapeutic agents is a global challenge for the scientific community. Despite of the emergence of MDR pathogens, the development of novel and more effective drugs is slow and scientist even speculate that we are going back the pre-antibiotic era. This work aims to study and evaluate the preliminary antibacterial, anthelmintic and cytotoxic potentials of ethyl 3-oxo-2-(2,5-dioxopyrrolidin-3-yl)butanoates. Among all of the four compounds, compound 2 has displayed remarkable potency with MIC values of 0.125, 0.083, 0.073, and 0.109 mg/ml against E. sakazakii, E. coli. S. aureus, and K. pneumonia, respectively. Compared to etoposide (LC50 9.8 μg/ml), the compounds demonstrated LC50 values from 280 to 765 μg/ml. For anthelmintic assay, three concentrations of each compound and standard drug were studied in determination of time of death of the two species. Excellent anthelmintic activity was observed by all four compounds against P. posthuma and A. galli better than standard albendazole. High GOLD fitness score data from docking analysis toward the targets represent better protein–ligand binding affinity and thus indicate a high propensity for all the active compounds to bind to the active site. The promising in-vitro antimicrobial, anthelmintic activity, and cytotoxicity data conclusively revealed that these compounds may serve as viable lead compounds for the treatment of bacterial and parasitic infections, and therefore, could help the medicinal chemists to design future chemotherapeutic agents to avoid rapid drug resistance.
Highlights
Microbial resistance and invading of infectious life-threatening diseases is a real challenge for scientists of the current era (Alanis, 2005; Ayaz et al, 2016a, 2017b)
To combat with the scenario of increasing over resistance of microorganisms, it is important to develop novel antibiotics preferably working with different mechanism of action (Kasanah and Hamann, 2004; Zeb et al, 2017)
We have shown that ketoester derivatives of Succinimides can be used as antibacterial, anthelmintic and cytotoxic agents
Summary
Microbial resistance and invading of infectious life-threatening diseases is a real challenge for scientists of the current era (Alanis, 2005; Ayaz et al, 2016a, 2017b). Synthesis and Biological Evaluation of Ethyl 3-oxo-2-(2,5-dioxopyrrolidin-3-yl)butanoate Derivatives agents and unavailability of resistance modifying antibiotics against MDR pathogens (Wise et al, 1998; Ayaz et al, 2016a). The antimicrobial agents can be obtained from synthetic or natural sources (Herrlich and Schweiger, 1976; Ayaz et al, 2015b; Kamal et al, 2015a; Shah et al, 2015). The synthetic drugs are normally accompanied with unwanted side effects while the natural drugs possess broad spectrum of pharmacological activities and are more safe (Ayaz et al, 2014a, 2015a, 2017a; Ahmad et al, 2015, 2016b; Kamal et al, 2015b; Ali et al, 2016, 2017; Zeb et al, 2016). There is a great need of new research for the development of new drugs which can be effective against several bacterial strains
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