Synthesis of osteotropic hydroxybisphosphonate derivatives of fluoroquinolone antibacterials

被引:53
|
作者
McPherson, James C., III [2 ]
Runner, Royce [2 ]
Buxton, Thomas B. [2 ]
Hartmann, John F. [3 ]
Farcasiu, Dan
Bereczki, Ilona [1 ]
Roth, Erzsebet [1 ]
Tollas, Szilvia [1 ]
Ostorhazi, Eszter [4 ]
Rozgonyi, Ferenc [4 ]
Herczegh, Pal [1 ]
机构
[1] Univ Debrecen, Dept Pharmaceut Chem, Med & Hlth Sci Ctr, H-4010 Debrecen, Hungary
[2] Eisenhower Army Med Ctr, Dept Clin Invest, Ft Gordon, GA USA
[3] ElizaNor Biopharmaceut Inc, Princeton Jct, NJ USA
[4] Semmelweis Univ, Dept Dermatol Venerol & Dermatooncol, Microbiol Lab, H-1085 Budapest, Hungary
关键词
Fluoroquinolone; Antibiotic; 1-Hydroxybisphosphonate; Osteotropic; Bone model; Adsorption; BONE RESORPTION; TISSUE CULTURE; BISPHOSPHONATES; PRODRUGS; OSTEOMYELITIS; DISSOLUTION; PREVENTION; DELIVERY; VITRO;
D O I
10.1016/j.ejmech.2011.10.049
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
1-Hydroxybisphosphonate derivatives of ciprofloxacin, gatifloxacin and moxifloxacin have been synthesized using Cu(I) catalyzed azide-alkyne 1,3-dipolar cycloaddition reaction. The 1,2,3-triazol linked hydroxybisphosphonate derivative of ciprofloxacin exhibited antibacterial activity comparable to the parent antibiotic and all fluoroquinolone-bisphosphonates displayed osteotropic properties in a bone model. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:615 / 618
页数:4
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