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Synthesis and biological evaluation of novel structural hybrids of benzofuroxan derivatives and fluoroquinolones.

Abstract：

:A series of novel hybrids based on benzofuroxan derivatives and fluoroquinolones (4a-d-6a-d) have been synthesized. Unexpectedly, the reactions have resulted in salt products formation during the hydrolysis of benzofuroxans by water molecules being present in the solvent instead of usual substitution products. All the compounds have been screened for antimicrobial and toxic activities. All resulting compounds retain high activity characteristic for fluoroquinolones. Many of the salts based on benzofuroxans and fluoroquinolones have higher activity than starting fluoroquinolones against Bacillus cereus 8035. Among the screened compounds, the compound 4d has shown the best antibacterial activity against B. cereus 8035, 8 times higher than the original Lomefloxacin (MBC value 1.5 μg/mL).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Chugunova E,Akylbekov N,Bulatova A,Gavrilov N,Voloshina A,Kulik N,Zobov V,Dobrynin A,Syakaev V,Burilov A

doi

10.1016/j.ejmech.2016.03.086

subject

Has Abstract

pub_date

2016-06-30 00:00:00

pages

165-172

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30268-9

journal_volume

116

pub_type

杂志文章

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