Structure-activity relationship study of homoallylamines and related derivatives acting as antifungal agents.
The synthesis, in vitro evaluation, and structure-activity relationship studies of homoallylamines and related derivatives acting as antifungal agents are reported. Among them, compounds N-(4-bromophenyl)-N-(2-furylmethyl)amine and N-(4-chlorophenyl)-N-(2-furylmethyl)amine reported here exhibited remarkable antifungal activity against dermatophytes. Theoretical calculations allow us to determine the minimal structural requirements to produce the antifungal response and can provide a guide for the design of compounds with these properties.
Suvire
Fernando D
FD
Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis (U.N.S.L.), Chacabuco 917, 5700 San Luis, Argentina.
Sortino
Maximiliano
M
Kouznetsov
Vladimir V
VV
Vargas M
Leonor Y
LY
Zacchino
Susana A
SA
Cruz
Uriel Mora
UM
Enriz
Ricardo D
RD
D000499:Allylamine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003883:Arthrodermataceae / Q000187:drug effects; D002478:Cells, Cultured; D003198:Computer Simulation; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D000499:Allylamine