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2005
Oxazole derivatives
R 0220
Effects of Positional and Geometrical Isomerism on the Biological Activity of
Novel Oxazolidinones. — Oxazolidinone derivatives [cf. (XI), (XII)] having
19- 136 Some
positional and geometrical substitution with various azole systems are synthesized by
Knoevenagel condensation reactions of aldehyde (IX) with acetonitrile derivatives (X).
Contrary to the expectations, none of these compounds shows antimycobacterial activity. However, some of them display antibacterial activity against Gram-positive pathogens. Thioacetamide (XII), the most potent compound amongst the molecules
screened, possesses good antibacterial activity comparable to linezolid. — (DAS*, J.;
et al.; Bioorg. Med. Chem. Lett. 15 (2005) 2, 337-343; Chem. Discovery Res., Dr.
Reddy's Lab. Ltd., Hyderabad 500 050, India; Eng.) — R. Staver
2005
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