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Antimycobacterial 3-phenyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-dithiones substituted on phenyl and benzoxazine moiety in position 6

✍ Scribed by Eva Petrlíková; Karel Waisser; Rafael Doležal; Pavel Holý; Jiří Gregor; Jiři Kuneš; Jarmila Kaustová

Book ID
111491460
Publisher
Versita
Year
2011
Tongue
English
Weight
266 KB
Volume
65
Category
Article
ISSN
0366-6352

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✦ Synopsis

Abstract

A series of forty-five derivatives of 3-phenyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and forty-five derivatives of 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-dithiones was synthesised. The compounds exhibited in-vitro activity against Mycobacterium tuberculosis, M. kansasii (two strains), and M. avium. The most active derivatives were more active than isonicotinhydrazide (INH). The quantitative relationships between the structure and antimycobacterial activity were calculated. The activity against M. tuberculosis increased with the lipophilicity of the substituents.

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