期刊
MOLECULES
卷 17, 期 11, 页码 13183-13198出版社
MDPI AG
DOI: 10.3390/molecules171113183
关键词
pyrazinamide analogues; lipophilicity determination; in vitro antimycobacterial; antifungal and photosynthesis inhibitory activity
资金
- GAUK [B-CH/710312]
- IGA NT [13346]
- Slovak Grant Agency VEGA [1/0612/11]
- Sanofi-Aventis Pharma Slovakia
- Education for Competitiveness Operational Programme (ECOP) [CZ.1.07/2.3.00/30.0022]
- European Social Fund
- state budget of the Czech Republic
- [SVV-2012-265-001]
A series of twelve amides was synthesized via aminolysis of substituted pyrazinecarboxylic acid chlorides with substituted benzylamines. Compounds were characterized with analytical data and assayed in vitro for their antimycobacterial, antifungal, antibacterial and photosynthesis-inhibiting activity. 5-tert-Butyl-6-chloro-N-(4-methoxybenzyl)pyrazine-2-carboxamide (12) has shown the highest antimycobacterial activity against Mycobacterium tuberculosis (MIC = 6.25 mu g/mL), as well as against other mycobacterial strains. The highest antifungal activity against Trichophyton mentagrophytes, the most susceptible fungal strain tested, was found for 5-chloro-N-(3-trifluoromethylbenzyl)-pyrazine-2-carboxamide (2, MIC = 15.62 mu mol/L). None of the studied compounds exhibited any activity against the tested bacterial strains. Except for 5-tert-butyl-6-chloro-N-benzylpyrazine-2-carboxamide (9, IC50 = 7.4 mu mol/L) and 5-tert-butyl-6-chloro-N-(4-chlorobenzyl)pyrazine-2-carboxamide (11, IC50 = 13.4 mu mol/L), only moderate or weak photosynthesis-inhibiting activity in spinach chloroplasts (Spinacia oleracea L.) was detected.
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