2-acetylpyridine thiosemicarbazones. 13. Derivatives with antifilarial activity.
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.
Klayman
D L
DL
Walter Reed Army Institute of Research, Division of Experimental Therapeutics, Washington, D.C. 20307.
Lin
A J
AJ
McCall
J W
JW
Wang
S Y
SY
Townson
S
S
Grögl
M
M
Kinnamon
K E
KE
D000818:Animals; D004285:Dogs; D005368:Filariasis / Q000188:drug therapy*; D005369:Filaricides / Q000138:chemical synthesis* / Q000627:therapeutic use; D005849:Gerbillinae; D007202:Indicators and Reagents; D008297:Male; D015394:Molecular Structure; D009068:Movement; D009854:Onchocerca / Q000187:drug effects / Q000502:physiology; D012664:Semicarbazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000494:pharmacology / Q000627:therapeutic use*; D013987:Ticks
D005369:Filaricides; D007202:Indicators and Reagents; D012664:Semicarbazones; D013882:Thiosemicarbazones; C033836:2-acetylpyridine thiosemicarbazone