title: Synthesis and antimicrobial activities of 7-O-modified genistein derivatives.
abstract: Three series of genistein derivatives with heterocycles were prepared, in which genistein and heterocyclic moieties were separated by 2-carbon, 3-carbon and 4-carbon spacers. Among the 33 compounds we prepared 11 of them (2c and 5a-j) are reported for the first time, while the preparation of 2a,b, 3a-j and 4a-j was reported in our recent paper. All the derivatives were screened for antibacterial (Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas fluorescence) and antifungal (Aspergillus niger, Candida albicans and Trichophyton rubrum) activities by MTT method. Among the compounds tested, 4a, 4e, 4f, 4h, 5e and 5f exhibited good antibacterial activities while 4a also showed notable antifungal activity. Especially, 5f exhibited stronger antibacterial activity against B. subtilis and S. aureus comparable to positive controls.
authors.affiliation: School of Life Sciences, Nanjing University, Nanjing, PR China.
authors.forename: Li-Na
authors.initials: LN
authors.lastname: Zhang
authors.forename: Ping
authors.initials: P
authors.lastname: Cao
authors.forename: Shu-Hua
authors.initials: SH
authors.lastname: Tan
authors.forename: Wen
authors.initials: W
authors.lastname: Gu
authors.forename: Lei
authors.initials: L
authors.lastname: Shi
authors.forename: Hai-Liang
authors.initials: HL
authors.lastname: Zhu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019833:Genistein / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000900:Anti-Bacterial Agents; D019833:Genistein