Abstract:
: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.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
McPherson JC 3rd,Runner R,Buxton TB,Hartmann JF,Farcasiu D,Bereczki I,Roth E,Tollas S,Ostorházi E,Rozgonyi F,Herczegh Pdoi
10.1016/j.ejmech.2011.10.049subject
Has Abstractpub_date
2012-01-01 00:00:00pages
615-8issue
1eissn
0223-5234issn
1768-3254pii
S0223-5234(11)00791-4journal_volume
47pub_type
杂志文章abstract::A novel series of 1,2,4-trioxanes were synthesized from 2H-pyrans via photooxidation, and their antiproliferative and growth factor inhibitory activity has been investigated across a variety of human cancer cell lines. Compounds 5k, 5l, 5s, 7a and 7c exhibited the highest activity and selectivity against a human leuke...
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abstract::The photophysical properties of naphthalimide-based fluorophores can be easily tuned by chemical manipulation of the substituents on that privileged scaffold. Replacement of a OMe group at position 6 in 2-(hydroxyl)ethyl-naphthalimide derivatives by diverse amines, including 2-(hydroxyl)ethylamine, trans-(4-acetamido)...
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abstract::Two series of peptidomimetics containing a novel C(2) pseudosymmetrical hydroxyalkyldiamino core structure were prepared from amino acid starting materials and tested for inhibitory activity against the HIV-1 protease (HIV-1 Pr) and the virus in cell culture. In the 2,3-diamino-1-hydroxypropane series, compound 6a, co...
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