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1,4‐Benzothiazine‐2‐carboxylic acid 1‐oxides as analogues of antibacterial quinolones
Author(s) -
Cecchetti Violetta,
Fravolini Arnaldo,
Schiaffella Fausto,
Tabarrini Oriana,
Zhou Weicheng,
Pagella Pier Giuseppe
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.5570290215
Subject(s) - benzothiazine , chemistry , quinolone , antibacterial activity , intramolecular force , carboxylic acid , combinatorial chemistry , organic chemistry , stereochemistry , bacteria , antibiotics , biochemistry , biology , genetics
The synthesis of 1,4‐benzothiazine‐2‐carboxylic acid 1‐oxides as agents which mimic quinolone antibacterial, are described. The key step includes intramolecular cyclization of phenylsulfinyl acrylates 17 and 18 which are prepared in six steps from 11. None of new target compounds showed interesting antibacterial activity in vitro against the tested strains.