Novel fluorescent risedronates: Synthesis, photodynamic inactivation and imaging of Bacillus subtilis

作者:Zhou, Li-Sheng; Yang, Ke-Wu*; Feng, Lei; Xiao, Jian-Min; Liu, Cheng-Cheng; Zhang, Yi-Lin; Crowder, Michael W.
来源:Bioorganic & Medicinal Chemistry Letters, 2013, 23(4): 949-954.
DOI:10.1016/j.bmcl.2012.12.051

摘要

Novel fluorescently-labeled conjugates of risedronate were synthesized using an epoxide linker, enabling conjugation of risedronate via its pyridyl nitrogen with the aromatic succinimidyl esters. The compounds were characterized by using H-1 NMR, C-13 NMR, P-31 NMR, UV-vis and fluorescence emission spectroscopies. Biological activity assays showed that the conjugates 14 and 15 exhibited photodynamic inactivation of Bacillus subtilis (ATCC 6633) with 91% and 47% bacterial lethality at 10 mu M upon visible light irradiation, respectively. Both 14 and 15 could be also used for fluorescence imaging of Bacillus subtilis.