Collect. Czech. Chem. Commun. 1984, 49, 285-294

Substituted 5- and 6-quinoxalinecarboxylic acids and their tuberculostatic activity

František Roubínek, Viktor Bydžovský and Zdeněk Buděšínský

Research Institute for Pharmacy and Biochemistry, 130 00 Prague 3


Condensation of aliphatic and aliphatic-aromatic α-diketones, and of substituted benzils with 2,3- and 3,4-diaminobenzoic acids and with 4,5-diamino-2-hydroxybenzoic acid gave 74 5- and 6-quinoxalinecarboxylic acids, with the same or different alkyls and aryls as substituents at position 2 and 3. The compounds with different substituents at positions 2 and 3 were resolved into positional isomers. Their structures were determined by means of the dipole moments. The compounds were tested for tuberculostatic activity. Some exhibited it in vitro (LI, LVII), but failed in vivo.