Antimicrobial Activities of Monoesters of Succinic Acid

Abstract

Fungi and bacteria are a great threat to all living organisms by causing illnesses in them. Rate of spreading diseases by them is higher in contrast to synthesis of drugs that are antifungal and/or antibacterial 1-4. At present substantial part of the research in chemistry is devoted to the synthesis and characterization of biologically active compounds that would be used against the microbes 5-16. Monoesters of succinic acid, in addition to their chemical uses, possess medicinal properties like, antiHIV, antitumor, antiseptic, antioxidant, antifungal and antibacterial 10-16 activities. In continuation to our work to establish medicinal use of monoesters 17-20 twentyseven (1-27) new monoesters were prepared from succinic anhydride 7 and explored for antifungal and antibacterial activity. All the reported compounds displayed considerable bioactivities. However, the halogenated esters displayed activity equivalent to standard drugs chloramphenicol and ketoconazole. EXPERIMENTAL The microbes used for bioactivities of synthesized compounds (1-27) were Candida albicans ATCC 10231 (C. albicans), Aspergillus niger F2723 (A. niger), Escherichia coli MTCC-739 (E. coli) and Proteus mirabilis ATCC 14153 (P. mirabilis). Ketoconazole purchased from M/s SMS Pharmaceuticals Ltd. Hyderabad and chloramphenicol from Sigma St. Louis, USA was used as standard.

Synthesis, Physico-Chemical and Antidiabetic Studies of Zinc Complex of Glimepiride, an Oral Hypoglycemic Agent

“…On refluxing the mixture content for 3hrs at 80 0 C and on cooling the off white coloured crystals were obtained. [14][15][16][17] Thecomplex was washed with 80% DMF or alcohol and weighed (yield-52%). …”

Evaluation of antifungal and antibacterial activities of monoesters of succinic anhydride

“…All the microbes were found to be sensitive towards compound 20 displaying MIC values 2.12-2.32 µg/mL. The study also showed that halogenated esters (12)(13)(14)(15)(16)(17)(18)(19) (1-8, 21-29) microbes were resistant and showed very small zone of inhibition (Table 1), whereas compounds 9-11 were almost inactive. The prepared compounds showed interesting structure activity relationships while exploring their antifungal and antibacterial activity.…”

“…In the last report the monoesters of succinic acid (1-29) were synthesised and characterised [19] whereas, in the present study the biological activities of these compounds (1-29) against various microbes are reported. All the reported compounds were bioactive, however, only the halogenated esters 11-20 displayed activity equivalent to standard drugs chloramphenicol and ketoconazole.…”

“…The aryl hydrogen succinates (1-29) were synthesized and characterised by following the standard protocol [19]. Briefly, 15 mmol of corresponding alcohol was added to succinic anhydride (15 mmol), anhydrous p-toluenesulfonic acid (0.06 mmol) and toluene (15 mL) under the atmosphere of nitrogen in a single-necked round-bottom flask (100 mL).…”

“…Therefore, quite a good number of scientists are involved in the synthesis of biologically active compounds and characterise them with reference to their antimicrobial properties [18][19][20]. In the last report the monoesters of succinic acid (1-29) were synthesised and characterised [19] whereas, in the present study the biological activities of these compounds (1-29) against various microbes are reported.…”