Abstract
Molecular hybridization has a wide application in medicinal chemistry to obtain new biologically active compounds. New isatin-indole molecular hybrids 5a–n have been synthesized and characterized by various spectroscopic tools. The in vitro antimicrobial potential of the prepared compounds 5a–n was assessed using diameter of the inhibition zone (DIZ) and minimum inhibitory concentration (MIC) assays against a panel of Gram-negative bacteria, Gram-positive bacteria and fungi. Most of the synthesized compounds 5a–n showed weak activities against Gram-negative bacteria while compounds 5b and 5c exhibited good activities against Gram-positive bacteria. On the other hand, compound 5j emerged as the most active compound towards Candida albicans (C. albicans), with an MIC value of 3.9 µg/mL, and compound 5g as the most active congener towards Asperagillus niger (A. niger), with an MIC value of 15.6 µg/mL. Moreover, compound 5h manifested the best anti-P. notatum effect, with an MIC value of 7.8 µg/mL, making it equipotent with compound 5g.
Highlights
Resistance to the currently available chemotherapeutic antimicrobial agents has become an attractive subject of interest over the past 10 years
The synthesis was commenced by esterification of the commercially available was commenced by esterification of the commercially available 5-methoxyindole-2-carboxylic acid
(1) in methanol in the presence of a catalytic amount of sulfuric acid according to the previouslyof sulfuric method acid according to the previously reported method [34]
Summary
Resistance to the currently available chemotherapeutic antimicrobial agents has become an attractive subject of interest over the past 10 years. Understanding antimicrobial drug resistance mechanisms plays a crucial role in developing effective therapeutic and prophylactic strategies to preclude the problems that are encountered with resistant pathogens. The development of antimicrobial resistance microbes might occur via upregulation of genes managing drug efflux, alteration of the structure or levels of the molecular targets, or decreased affinity of the antimicrobial agents for their targets. Isatin (I, 1H-indole-2,3-dione; Figure 1) is a heterocyclic compound that was first synthesized nearly 170 years ago by Erdmann and Laurent [4,5]. Thereafter, it has been identified as an endogenous multifunctional compound in plants [6], fungi [7], marine organisms [8], and mammals [9]
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