Klayman D L, Lin A J, McCall J W, Wang S Y, Townson S, Grögl M, Kinnamon K E
Walter Reed Army Institute of Research, Division of Experimental Therapeutics, Washington, D.C. 20307.
J Med Chem. 1991 Apr;34(4):1422-5. doi: 10.1021/jm00108a027.
Several members of a series of 2-acetylpyridine thiosemicarbazones possess in vivo and in vitro macrofilaricidal properties. The most promising of the group tested is N4-(2-aminophenyl)-2-[1-(2-pyridinyl)ethylidene]-hydrazinecarbothioam ide (4), which suppressed 100% of the macrofilariae of Brugia pahangi and 94% of those of Acanthocheilonema viteae in the jird at a dose of 25 mg/kg per day x 5. Compounds 4 and 14 were also shown to inactivate or kill Onchocerca gutturosa and Onchocerca volvulus adult worms as measured by the loss of their motility or the inhibition of the conversion by the worms of the dye MTT to formazan.
一系列2-乙酰吡啶硫代半卡巴腙的几个成员具有体内和体外杀大丝虫特性。该组中最有前景的测试化合物是N4-(2-氨基苯基)-2-[1-(2-吡啶基)亚乙基]-肼基硫代甲酰胺(4)，以每天25mg/kg的剂量×5给药时，它能抑制沙鼠体内100%的彭亨布鲁线虫大丝虫和94%的旋盘尾丝虫大丝虫。化合物4和14还显示能使喉盘尾丝虫和旋盘尾丝虫成虫失活或杀死，这通过成虫运动能力丧失或对染料MTT转化为甲臜的抑制来衡量。
