期刊
MOLECULES
卷 17, 期 1, 页码 613-644出版社
MDPI
DOI: 10.3390/molecules17010613
关键词
quinolines; naphthalene; lipophilicity; photosynthetic electron transport inhibition; spinach chloroplasts; in vitro antimycobacterial activity; in vitro cytotoxicity
资金
- IGA VFU [Brno 49/2011/FaF]
- Slovak Grant Agency VEGA [1/0612/11]
- Sanofi-Aventis Pharma Slovakia
- Irish Department of Agriculture Fisheries and Food [08RDCIT601]
In this study, a series of thirty-five substituted quinoline-2-carboxamides and thirty-three substituted naphthalene-2-carboxamides were prepared and characterized. They were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial species. N-Cycloheptylquinoline-2-carboxamide, N-cyclohexylquinoline-2-carboxamide and N-(2-phenylethyl)quinoline-2-carboxamide showed higher activity against M. tuberculosis than the standards isoniazid or pyrazinamide and 2-(pyrrolidin-1-ylcarbonyl)quinoline and 1-(2-naphthoyl)pyrrolidine expressed higher activity against M. kansasii and M. avium paratuberculosis than the standards isoniazid or pyrazinamide. The most effective antimycobacterial compounds demonstrated insignificant toxicity against the human monocytic leukemia THP-1 cell line. The PET-inhibiting activity expressed by IC50 value of the most active compound N-benzyl-2-naphthamide was 7.5 mu mol/L. For all compounds, the structure-activity relationships are discussed.
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