Ram V J, Mishra L, Kushwaha D S
Arch Pharm (Weinheim). 1989 Feb;322(2):63-6. doi: 10.1002/ardp.19893220202.
4-Amino-3-hydrazino-5-H/methyl-1,2,4-triazole dihydrochlorides (2a,b) were obtained by cyclization of triamino-guanidine-HCl in formic and acetic acids, respectively. Condensation of 2a with pyrazol-4-carbaldehydes in ethanol yielded 3a,b. Cyclocondensation of 2a,b with dimethylmercaptocyanoacrylonitrile, methyl dimethylmercapto-cyanoacrylate, ethoxymethylenemalononitrile and ethyl ethoxymethylenecyanoacetate individually provided 4a-d and 5a-d, respectively. The hydrazones 6a,b were obtained by refluxing 4-amino-3-(5-amino-4-ethoxycarbonyl pyrazol-1-yl)-1,2,4-triazole (5b) with aryl aldehydes in ethanol. Interaction of 2a with acetylacetone and 2-ethoxycarbonylcyclopentanone separately yielded 7 and 8 while reaction with 2-ethoxycarbonylcyclohexanone provided the bicyclic compounds 9a,b. Some of the compounds were screened for antibacterial and antifungal activities but none of them showed any significant activity.
4-氨基-3-肼基-5-H/甲基-1,2,4-三唑二盐酸盐（2a,b）分别通过三氨基胍盐酸盐在甲酸和乙酸中环化得到。2a与吡唑-4-甲醛在乙醇中缩合得到3a,b。2a,b分别与二甲基巯基氰基丙烯腈、甲基二甲基巯基氰基丙烯酸酯、乙氧基亚甲基丙二腈和乙氧基亚甲基氰基乙酸乙酯进行环缩合反应，分别得到4a-d和5a-d。腙6a,b是通过4-氨基-3-(5-氨基-4-乙氧羰基吡唑-1-基)-1,2,4-三唑（5b）与芳醛在乙醇中回流得到的。2a分别与乙酰丙酮和2-乙氧羰基环戊酮反应得到7和8，而与2-乙氧羰基环己酮反应得到双环化合物9a,b。对部分化合物进行了抗菌和抗真菌活性筛选，但均未显示出任何显著活性。
