ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

Newly synthesized indolizine derivatives – antimicrobial and antimutagenic properties

Petra Olejníková, Lucia Birošová, Ľubomír Švorc, Zuzana Vihonská, Martina Fiedlerová, Štefan Marchalín, and Peter Šafář

Department of Biochemistry and Microbiology, Institute of Biochemistry, Nutrition and Health Protection

E-mail: petra.olejnikova@gmail.com

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).

Keywords: indolizine derivative – antimicrobial activity

Full paper is available at www.springerlink.com.

DOI: 10.1515/chempap-2015-0093

Chemical Papers 69 (7) 983–992 (2015)