SAR Oxazoles The triazole or imidazole ring are essential for the activity, the N-3 atom of azole ring binds to the ferric iron atom in the heme the varying of R, and R, can bel prosthetic group to provent the activation RI=OHN Or R R2 formed a 1,3 of oxygen for insertion ino lanosterol dioxapetane The activity: X-N>X-CH R (CH2)n-C-R The substitution must on the N-I, other position will lose he activity The 2,4 position of aromatic ring are intruduced eletron-withdrawin group, such as, F, CI, will increase antifungal activitySAR of Azoles N X N (CH2 )n C R1 R2 Ar The triazole or imidazole ring are essential for the activity, the N 3 binds to the ferric iron atom in the heme prosthetic group to provent the activation of oxygen for insertion ino lanosterol. The activity: X=N > X=CH atom of azole ring 1 The substitution must on the N ,other position will lose the activity The 2 ,4 position of aromatic ring are intruduced eletron withdrawing group,such as, F,Cl, will increase antifungal activity. the varying of R1 and R2 can be : R1= OH, or R, R2 formed a 1,3 dioxapetane