Abstract:
:We report in this work the synthesis, cytotoxicity, and antimicrobial activity of ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acid amides 4-7 in connection with our previous research in the preparation of triazoloquinazoline derivatives. Due to simplicity, general availability of starting materials, and high yields, the most reliable method of synthesis appeared to be the one with N,N-carbonyldiimidazole activation stage. The chemical structures of all obtained substances were deduced from FT-IR, (1)H-NMR, EI-MS, and LC-MS spectral data. The results of cytotoxicity evaluated by bioluminescence inhibition of bacterium Photobacterium leiognathi, strain Sh1 showed that compounds 4.1, 4.6, and 6.1 were the most cytotoxic. Investigation of the antimicrobial and antifungal activity of amides 4-7 (concentration 5 mg/mL) was carried out by the stiff-plate agar-diffusion method. We found that the compounds possessed low (4.1, 4.7) antifungal activity against Candida tenuis and strong (4.21, 5.1, 5.9) or inefficient (4.7, 4.12, 4.16) activity against Aspergillus niger. Substances 5.1 and 5.9 slightly affected Mycobacterium luteum. Staphylococcus aureus was resistant to all obtained substances, and only the n-butyramide derivatives 7.1 and 7.5 inhibited the growth of Escherichia coli. Hence, there was no strong correlation between bioluminescence inhibition and antimicrobial activity of the investigated substances.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Antipenko LN,Karpenko AV,Kovalenko SI,Katsev AM,Komarovska-Porokhnyavets EZ,Novikov VPdoi
10.1002/ardp.200900077subject
Has Abstractpub_date
2009-11-01 00:00:00pages
651-62issue
11eissn
0365-6233issn
1521-4184journal_volume
342pub_type
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