Antimicrobial activity of some substituted triazoloquinazolines.

Fifteen substituted 1,2,4-triazolo[4,3-c]quinazolines were tested for antibacterial and antifungal effects. The most effective derivatives had the triazoloquinazoline skeleton substituted with the pharmacologically active chromophores--morpholine, chlorine and nitro group. The broadest antimicrobial activity was found with 5-morpholin-4-yl-3-(5-nitrothien-2-yl)[1,2,4]triazolo[4,3-c]quinazoline in concentration of 10 mg/L for B.

Biological activity of some 4-anilinoquinazolines: cytotoxic, genotoxic and antiprotease effects, induction of necrosis and changes of actin cytoskeleton.

Fourteen substituted 4-anilinoquinazolines have been tested for cytotoxic effect and structure activity relationships. The most active derivatives were substituted by chlorine or bromine group in the aromatic ring, in the pyrimidine ring by morpholine group and in the aniline skeleton by nitro group in position 4 or 2. Derivatives 6-bromo-2-(morpholin-1-yl)-4-(4'-nitroanilino)quinazoline, 6-bromo-2-morpholin-1-yl)-4-anilinoquinazoline, 2-(morpholin-1-yl)-4-(4'-bromoanilino)-quinazoline and 6-chloro-2-(morpholin-1-yl)-4-(4'-nitroanilino)quinazoline inhibited growth of tumor cell lines HeLa, B16 and L1210.

Antibacterial effects of trisubstituted quinazoline derivatives.

Five trisubstituted quinazolones and eight trisubstituted quinazoline-4-thiones have been tested for antibacterial effects by a microdilution method. Four derivatives exerted a significant effect on E. coli, P.

[Antibacterial and antineoplastic activity of 2,4-disubstituted 6H-5,1,3-benzothiadiazocines].

Nine 2,4-disubstituted 6H-5,1,3-benzothiadiazocines have been tested for antibacterial and cytotoxic efficacy. None of the tested compounds showed any significant antibacterial activity in comparison with ampicillin. The most cytotoxic effect was manifested by those derivatives which have morpholine or phenyl in position 2 and benzimidazole, imidazole or 1,2,4-triazole in position 4.

Antibacterial effect of some substituted tricyclic quinazolines and their synthetic precursors.

Eleven substituted tricyclic quinazolines and their synthetic precursors were tested for antibacterial effects. 3-Chloromethylcarbonyl-2-methylquinazolin-4-thione and 5-phenyl-2,3-dihydro-1,2,4-triazolo[4,3-c]quinazolin-3-one had the highest antibacterial effect against Bacillus subtilis, the MIC values being 50 mg/L. Two tested derivatives were more active against Pseudomonas aeruginosa than ampicillin, the IC50 values being 80 and 100 mg/L.