New heterocyclic derivatives of benzimidazole with germicidal activity--XI--Experimental validation of OSAR prediction on antibacterial and antimycotic activity of benzimidazole derivatives.
In continuation of previous studies, Authors describe the synthesis of three new derivatives of 2-(5'-nitro-2'-furyl) benzimidazole, having hydroxy, methoxy or amino group at position 5. The new compounds, synthesized as suggested by a previous chemometric study, were tested in vitro against 5 Gram + and 4 Gram- strains and the mycete C. albicans. Two derivatives (R = OH, NH2) showed a good degree of antibacterial activity, especially the 5-hydroxy derivative, but they were practically inactive against the mycete; these results are in agreement with the prediction of chemometric study.
Pedini
M
M
Istituto di Biochimica e Chimica Medica, Facoltà di Medicina e Chirurgia, Università degli Studi di Perugia, Italia.
De Meo
G
G
Ricci
A
A
Bastianini
L
L
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D001562:Benzimidazoles