1326237-15-3Relevant academic research and scientific papers
Synthesis and antitrypanosomal activities of novel pyridylchalcones
Bhambra, Avninder S.,Ruparelia, Ketan C.,Tan, Hoon L.,Tasdemir, Deniz,Burrell-Saward, Hollie,Yardley, Vanessa,Beresford, Kenneth J.M.,Arroo, Randolph R.J.
, p. 213 - 218 (2017)
A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC50value of 0.29?μM. Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47. Little activity was seen when the library was tested against Leishmania donovani. In conclusion, pyridylchalcones are promising leads in the development of novel compounds for the treatment of human African trypanosomiasis (HAT).
Synthesis and antimicrobial activity of methoxy azachalcones and N-Alkyl substituted methoxy azachalconium bromides
Albay, Canan,Kahriman, Nuran,Yilmaz Iskender, Nagihan,Alpay Karaoglu, Senguel,Yayli, Nurettin
scheme or table, p. 441 - 454 (2012/02/02)
In this study, 18 new N-octyl, N-decyl, and N-dodecyl substituted o-, m-, and p-methoxy (E)-3-and 4-azachalcones, {4-or 3-[(1E)-3-(4-, 3-, or 2-methoxyphenyl)-3-oxoprop-1-en-1-yl]-1-alkyl (C8,10,12) pyridinium bromides} (1a-6a, 1b-1b, and 1c-6c), and 4 new o-, and m-methoxy (E)-3-and 4-azachalcones (2, 3, 5, and 6) were synthesized and tested for antimicrobial activities against Escherichia coli, Yersinia pseudotuberculosis, Enterobacter aerogenes, Pseudomonas aeruginosa, Staphylococcus aureus, Enterococcus faecalis, Bacillus cereus, and Candida albicans. N-Alkyl substituted azachalconium bromides showed good antimicrobial activity against all tested microorganisms with minimal inhibitory concentration (MIC) values in the range of 0.42-58.7 μg/mL in most cases. Nonalkylated compounds 1-9 were not as effective as the alkylated compounds. They showed only antimicrobial activity against gram-positive bacteria and yeast in the range of 1.77-123.7 μg/mL. The optimum length of the alkyl chain for better activity is situated with 12 carbon atoms in the series of compounds 1a-c, 2a-c, 3a-c, 4a-c, 5a-c, and 6a-c. N-Alkyl derivatives of m-methoxy (E)-3-azachalcone (4a-c, 5a-c, and 6a-c) showed better activity in comparison to those of oand p-methoxy (E)-4-azachalcones (1a-c, 2a-c, and 3a-c). TUeBITAK.
