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Relationships Between the Chemical Structure of Antimycobacterial Substances and Their Activity Against Atypical Strains. Part 14: 3‐Aryl‐6,8‐dihalogeno‐2 H ‐1,3‐benzoxazine‐2,4(3 H )‐diones
Author(s) -
Waisser Karel,
Hladuvková Jana,
Gregor Jirí,
Rada Tomáš,
Kubicová Lenka,
Klimešová Vera,
Kaustová Jarmila
Publication year - 1998
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/(sici)1521-4184(199801)331:1<3::aid-ardp3>3.0.co;2-2
Subject(s) - antimycobacterial , aryl , chemical structure , chemistry , stereochemistry , structure–activity relationship , chemical synthesis , biological activity , combinatorial chemistry , organic chemistry , mycobacterium tuberculosis , biochemistry , tuberculosis , medicine , in vitro , alkyl , pathology
A set of eight derivatives of 6,8‐dichloro‐3‐phenyl‐2 H ‐benzoxazine‐2,4(3 H )‐dione and nine derivatives of 6,8‐dibromo‐3‐phenyl‐2 H ‐1,3‐benzoxazine‐2,4(3 H )‐dione, substituted on the phenyl ring, was prepared by the reaction of the corresponding salicylanilides with ethyl chloroformate. The compounds were evaluated in vitro for antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii , and Mycobacterium avium . Their activity increases with increasing hydrophobicity and electron‐withdrawing ability of the substituents on the phenyl ring.