Abstract
Three series of isatin derivatives [3-hydrazino, 3-thiosemicarbazino, and 3-imino carboxylic acid derivatives] were synthesized employing microwave irradiation. The prepared compounds were characterized by FT-IR, NMR, elemental analysis, and X-ray crystallography for derivatives5b. The synthesized compounds were screened for antimicrobial activity against selected bacteria and fungi. The results revealed that theN-alkyl isatin derivatives were biologically active with different spectrums activity. Most of the 3-hydrazino and 3-thiosemicarbazino isatin derivatives were biologically inactive and generally the active derivatives showed weak to moderate activity mainly against Gram-positive bacteria. The imino isatin carboxylic acid derivatives (2-[4-(1-benzyl-5-bromo-2-oxoindolin-3-ylideneamino) phenyl]acetic acid,5d) showed promising activity against all tested Gram-positive bacteria and against fungal pathogens.
Highlights
The development of new therapeutic agents is one of the essential goals in medicinal chemistry
In the recent years there has been a spectacular increase in the use of microwave heating within the pharmaceutical industry, because it facilitates the synthesis of new chemical entities with reduced reaction time [1]
N-alkyl isatin derivatives 1b–1f were prepared from isatin derivatives according to the reported method employing microwave irradiation [30]
Summary
The development of new therapeutic agents is one of the essential goals in medicinal chemistry. In the recent years there has been a spectacular increase in the use of microwave heating within the pharmaceutical industry, because it facilitates the synthesis of new chemical entities with reduced reaction time [1]. Isatin is considered as important class of bioactive compounds exhibiting caspase inhibitor [12, 13], antibacterial, and antiproliferative activity [14]. Isatin derivatives reported to show antiviral [17], antiinflammatory, analgesic [18], and anticonvulsant activities [19]. Isatin-β-thiosemicarbazone derivatives were found to demonstrate a range of chemotherapeutic activities [20,21,22,23,24,25,26]. We report here the synthesis of three different series of isatin derivatives (hydrazone, thiosemicarbazone, and imino carboxylic acid derivatives) employing microwave irradiation. The prepared compounds were subjected to in vitro screening for their antimicrobial activities against representatives of pathogenic Gram-positive and Gram-negative bacteria and fungi
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