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Synthesis and Biological Activity of Tetrahydropyrido[2′,3′:4,5]imidazo[1,2‐ c ]pyrimidine‐6,8‐diones
Author(s) -
Sraga Jan,
Guerry Philippe,
Kompis Ivan
Publication year - 1994
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.19940770419
Subject(s) - chemistry , dna gyrase , pyrimidine , antibacterial activity , stereochemistry , in vitro , biological activity , dna , combinatorial chemistry , biochemistry , escherichia coli , bacteria , gene , genetics , biology
Substituted 4‐oxoquinoline‐3‐ ( 1a ) and 4‐oxo‐1,8‐naphthyridine‐3‐ ( 1b ) carboxylic acids are clinically useful antibacterial agents exerting their activity by inhibiting the subunit A of DNA gyrase. Recently, pyrimido‐[1,6‐ a ]benzimidazoles 2 were found to be a new class of inhibitors of this enzyme. As, in 1 , replacement of C(8) by the N‐atom was shown beneficial for the biological properties, a synthesis of the corresponding aza analogues of 2 has been carried out. The synthesis, DNA gyrase inhibitory activity, and in vitro antibacterial activity of the target compounds 16–19 are reported.