Premium
The Oriented Development of Antituberculotics (Part II): Halogenated 3‐(4‐Alkylphenyl)‐1,3‐benzoxazine‐2,4‐(3 H )‐diones
Author(s) -
Waisser Karel,
Matyk Josef,
Divišová Hana,
Husáková Petra,
Kuneš Jirí,
Klimešová Vera,
Palát Karel,
Kaustová Jarmila
Publication year - 2007
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/ardp.200600002
Subject(s) - chemistry , in vitro , stereochemistry , organic chemistry , medicinal chemistry , biochemistry
Based on our previous studies, 21 new halogenated 3‐(4‐alkylphenyl)‐1,3‐benzoxazine‐2,4‐(3 H )‐diones were synthesized by the reaction of salicylanilides and methyl‐chloroformate. All compounds were screened in vitro against three different strains of mycobacterium, and Free‐Wilson method was used to establish structure‐activity relationships. 6‐Bromo‐3‐(4‐butylphenyl)‐1,3‐benzoxazine‐2,4‐(3 H )‐dione 3b proved to be the most active compound of the series.