- Deacetylcolchicine deriv.
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Provided are 4-modified colchicine compounds and medicines using the same. Specifically provided are colchicine derivatives represented by general formula (1), salts thereof, and solvates of the same. In general formula (1), R1 is a halogen atom, a hydroxyl group, a nitro group, an amino group, or a mono-, di- or tri-fluoromethyl group; R2, R3 and R4 are each a methoxy group or a hydroxyl group, or alternatively R2 and R3, or R3 and R4 together represent a methylenedioxy group; R5 and R6 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, an arylalkyl group, a C2-6 alkenyl group, -COR7, -COOR8, -SO2R9, -CONR10R11, or -CSNR12R13, or alternatively R5 and R6 together with the nitrogen atom to which R5 and R6 are bonded may form a three- to seven-membered cyclic amino group; R7 is a C1-6 alkyl group or the like; R8 is a C1-6 alkyl group or the like; R9 is a C1-6 alkyl group or the like; R10 and R11 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, or the like; and R12 and R13 may be the same or different and are each a hydrogen atom, an alkyl group, or the like.
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Paragraph 0111
(2016/10/08)
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- Studies in Potential Filaricides: Part 19 - Synthesis of 1-Methyl-4-substituted Carbonylpiperazines as Diethylcarbamazine Analogs
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The synthesis and antifilarial activity of a series of 1-methyl-4-substituted carbamoyl- and carbonylpiperazines (6 - 42) against Litomosoides carinii in cotton rats and Dipetalonema viteae in Mastomys natalensis are described.The most potent compound of this series, 1-methyl-4-(pyrrolidin-1-yl)carbonylpiperazine (7) causes 95 - 98 percent reduction of blood microfilarial count in cotton rats infected with L. carinii at an intraperitoneal or oral dose of 1.5 (base) or 3 (citrate) mg/kg given for 6 days.A number of other compounds also exhibit marked microfilaricidal efffect in the dose range of 6 - 30 mg/kg.
- Sharma, Satyavan,Agarwal, V. K.,Dubey, S. K.,Iyer, R. N.,Anand, Nitya,et al.
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p. 748 - 751
(2007/10/02)
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