N-substituted 2-isocyanoarylacetamides with antimicrobial activity.
In this study, N-substituted 2-formylaminoarylacetamides (3) were obtained by the Ugi four-component reaction between isocyanides (1), aldehydes (2), and ammonium formate. The reaction products (3) were dehydrated with POCl3/NEt3 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 E. coli and fairly active against K. pneumoniae and S. aureus. A better activity was shown against B. subtilis, but all the tested compounds showed a very good inhibitory effect against C. albicans.
Bossio
R
R
Dipartimento di Chimica Organica, Ugo Schiff, Università di Firenze, Italy.
Marcaccini
S
S
Pellegrini
G
G
Pepino
R
R
D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000081:Acetamides; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents