Newly synthesized indolizine derivatives – antimicrobial and antimutagenic properties

Abstract

A series of indolizine derivatives have been synthesized and subjected to antibacterial screening studies. Antibacterial activity of 21 derivatives was investigated against Staphylococcus aureus, Mycobacterium smegmatis, Salmonella typhimurium and Escherichia coli; also, the sensitivity of model yeast Candida parapsilosis and some model filamentous fungi Aspergillus fumigatus, Alternaria alternata, Botrytis cinerea and Microsporum gypseum was tested. Newly synthesized indolizine derivatives have shown selective toxicity to Gram-positive bacteria S. aureus and were also considered to be able to inhibit the acidoresistant rod M. smegmatis. Derivative XXI has shown the highest inhibition effect with the bacteriostatic effect on the cells at the concentration of 25 µg mL −1 . The best antifungal activity has been detected in the presence of derivative XIII. Derivative XIII did also affect the morphology of hyphal tips of B. cinerea, which led to enhanced ramification of hyphae. Finally, the antimutagenic activity of derivatives was investigated. Significant antimutagenic activity was registered in case of derivative VIII. The number of induced revertants by mutagen [2-(5-nitrofuryl)acrylic acid] was decreased almost to the level of spontaneous revertants in the lowest applied concentration (50 µg per plate).

Resistance associated metabolite profiling of Aspergillus leaf spot in cotton through non-targeted metabolomics

“…Resistant cultivar infected with pathogen also depicted higher accumulation of alkaloids including 7-Hydroxydehydroglaucine, Indolizine, Benzosimuline, Acetylcorynoline, Flazine, Benzosimuline and Cepharadione A. These compounds have been reported for their antifungal activities [49,50,51,52]. In this study, numerous membrane glycerolipids including several PE (Phosphatidylethanolamine), PC (Phosphatidylcholine), PI (Phosphatidylinositol), PA (Phosphatidic acid), PIP (Phosphatidylinositol Phosphate), PS (Phosphatidylserine) and phosphocholine were also identified.…”

Polybenzimidazole-Triphenylphosphene-Catalyzed One-Pot Synthesis and Evaluation of Dihydropyridine Derivative as Antibiotics and Antifungals

“…Even then, there are number of drawbacks such as cost of the production, toxicity of catalyst, elevated temperature, low yields, environmental concern and finite scope on substrates. In the following synthetic methods such as using EtOH as solvent, solid phase synthesis, water as solvent, PEG‐400 as solvent and solvent‐free conditions at 40 °C, have been attempted. Even then the researchers are interested in the developing novel methods for the synthesis of dihydropyridines derivatives due to their prevalence in pharmaceutical agents.…”

Current Trends and Future Perspectives of Antimutagenic Agents

“…A series of indolizine derivatives have been synthesized to determine their antimutagenic activity, the indolizine derivative (Figure 22) had the highest activity [51].…”