20.500.12556/RUL-129246 Antimicrobial activity of the marine alkaloids, clathrodin and oroidin, and their synthetic analogues Marine organisms produce secondary metabolites that may be valuable for the development of novel drug leads as such and can also provide structural scaffolds for the design and synthesis of novel bioactive compounds. The marine alkaloids, clathrodin and oroidin, which were originally isolated from sponges of the genus, Agelas, were prepared and evaluated for their antimicrobial activity against three bacterial strains (Enterococcus faecalis, Staphylococcus aureus and Escherichia coli) and one fungal strain (Candida albicans), and oroidin was found to possess promising Gram-positive antibacterial activity. Using oroidin as a scaffold, 34 new analogues were designed, prepared and screened for their antimicrobial properties. Of these compounds, 12 exhibited >80% inhibition of the growth of at least one microorganism at a concentration of 50 µM. The most active derivative was found to be 4-phenyl-2-aminoimidazole 6h, which exhibited MIC$_{90}$ (minimum inhibitory concentration) values of 12.5 µM against the Gram-positive bacteria and 50 µM against E. coli. The selectivity index between S. aureus and mammalian cells, which is important to consider in the evaluation of a compound's potential as an antimicrobial lead, was found to be 2.9 for compound 6h. marine alkaloid Agelas antimicrobial antibacterial antifungal pyrrole-2-aminoimidazole oroidin clathrodin morski organizmi bioaktivne substance protimikrobne učinkovine protibakterijsko delovanje true false true Angleški jezik Slovenski jezik Članek v reviji 2021-08-31 10:08:00 2021-08-31 10:08:05 2022-09-08 04:07:29 0000-00-00 00:00:00 2014 0 0 Str. 940-963 iss. 2 Vol. 12 2014 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 577.1 1660-3397 10.3390/md12020940 3602801 RAZ_Zidar_Nace_2014.pdf RAZ_Zidar_Nace_2014.pdf 1 A060A14C95D26F61499CBC125476F811 a56e26dd0a29bc9e5c3a02faab59e2e5bf2040cd0242c9eaad452f3d092bcfb5 8b92acd9-0a32-11ec-a523-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=146209 http://www.mdpi.com/1660-3397/12/2/940 1 576f337c-0a32-11ec-a523-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=146208 Fakulteta za farmacijo 0 0 0