ニトロフラン系化合物の薬学的研究 (第9報)

ニトロフラン核を有する2-Amino-1,3,4-oxadiazole系化合物の合成ならびに構造活性相関について

抄録

2-Amino-5-(5-nitro-2-furylalkenyl)-1, 3, 4-oxadiazoles (IV) were prepared by the known methods and their antibacterial activity was tested.
IV was less effective than 3-amino-6-(5-nitro-2-furylalkenyl)-1, 2, 4-triazines (II), but their structure-activity relationship was quite similar to that of II. IV (R₁=H, n=0) was reacted with excess formaldehyde and 2-[bis(hydroxymethyl)amino]-5-[2-(5-nitro-2-furyl)vinyl]-1, 3, 4-oxadiazole (XVI) was obtained.
The protective effect of XVI in mice was tested and it was found to have stronger in vivo activity than 3-[bis(hydroxymethyl)amino]-6-[2-(5-nitro-2-furyl)vinyl]-1, 2, 4-triazine (I).