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The synthesis and biological activity of new 7‐[2‐(cyanomethyl)piperazinyl]‐ and 7‐[3‐(cyanomethyl)piperazinyl]quinolone antibacterials
Author(s) -
Gubert S.,
Braojos C.,
Anglada L.,
Bolós J.,
Palacin C.
Publication year - 1992
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570290108
Subject(s) - chemistry , quinolone , piperazine , antibacterial activity , regioselectivity , stereochemistry , combinatorial chemistry , antibiotics , organic chemistry , bacteria , catalysis , biochemistry , biology , genetics
Some novel 7‐[2‐ or 3‐(cyanomethyl)piperazinyl]quinolones have been prepared. Most notable, 2‐cyanomethyl‐piperazine 5 and 1‐methyl‐2‐cyanomethylpiperazine 8 at the quinolone C‐7 position produce products with good in vitro antibacterial activity. The key step in the synthesis of these products involves the regioselective deprotection of the benzyl group in function of the time reaction.