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N-substituted 2-isocyanoarylacetamides with antimicrobial activity

Bossio, R.; Marcaccini, S.; Pellegrini, G.; Pepino, R.

Arzneimittel-Forschung 42(12): 1494-1497

1992

ISSN/ISBN: 0004-4172
PMID: 1288515
Document Number: 404004
In this study, N-substituted 2-formylaminoarylacetamides (3) were obtained by he Ugi four-component reaction between isocyanides (1), aldehydes (2), and ammonium formate. The reaction products (3) were dehydrated with POCl-3/NEt-3 to give the title compounds (4). The structure of the compounds 3 and 4 was confirmed by spectral data and elemental analysis. Tests of antimicrobial activity showed that compounds 4 were ineffective against Escherichia coli and fairly active against Klebsiella pneumoniae and Staphylococcus aureus. A better activity was shown against Bacillus subtilis, but all the tested compounds showed a very good inhibitory effect against Candida albicans.

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