- DIHYDROOROTIC ACID DEHYDROGENASE INHIBITOR
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The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor which is applicable to various diseases. When used as an active ingredient, a compound represented by formula (I): (wherein X represents a halogen atom, R1 represents a hydrogen atom, R2 represents an alkyl group containing 1 to 7 carbon atoms, R3 represents -CHO, and R4 represents -CH2-CH=C(CH3)-R0 (wherein R0 represents an alkyl group containing 1 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon, etc.)), an optical isomer thereof or a pharmaceutically acceptable salt thereof has a high inhibitory effect on dihydroorotic acid dehydrogenase and can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anticancer agent, a therapeutic agent for graft rejection, an antiviral agent, an anti-H. pylori agent, a therapeutic agent for diabetes or the like.
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- NOVEL DIHYDROXYBENZENE DERIVATIVES AND ANTIPROTOZOAL AGENT COMPRISING SAME AS ACTIVE INGREDIENT
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Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents -CHO, -C(=O)R5, -COOR5 (wherein R5 represents a C1-7 alkyl group), -CH2OH or -COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.
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- A short and efficient total synthesis of (±)-ascofuranone
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Ascofuranone is a potent inhibitor of trypanosome alternative oxidase. A short and efficient total synthesis of (±)-ascofuranone was accomplished in only seven steps starting with geranyl acetate. The synthetic concept and methodology described in detail
- Haga, Yasushi,Tonoi, Takayuki,Anbiru, Yoshihide,Takahashi, Yuki,Tamura, Sayuri,Yamamoto, Masaichi,Ifuku, Shinsuke,Morimoto, Minoru,Saimoto, Hiroyuki
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p. 622 - 623
(2011/01/07)
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- Total synthesis of dl-ascofuranone and related compounds
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Convergent synthesis of an antitumor protective agent, ascofuranone, was accomplished by (1) preparation of the terpenoid side chain having a furanone moiety, (2) coupling the side chain with a protected phenol derivative, and (3) deprotection to regenerate the hydroxyl groups. This strategy was successfully applied to the synthesis of oxidized and cyclized analogs of ascofuranone. Some of the ascofuranone derivatives were found to inhibit the growth of P388 leukemia cells.
- Saimoto,Ohrai,Sashiwa,Shigemasa,Hiyama
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p. 2727 - 2734
(2007/10/03)
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- A MILD PROCEDURE FOR HYDROLYSIS OF ALKOXYMETHYL ARYL ETHERS TO GIVE HYDROXYARENES. A RATIONAL SYNTHESIS OF ASCOFURANONE
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A mild procedure is reported for cleavage of alkoxymethyl aryl ethers with P2I4 to afford hydroxyarenes, and this deprotection method was successfully applied to the synthesis of an antibiotic ascofuranone through a rational approach.
- Saimoto, Hiroyuki,Kusano, Yukari,Hiyama, Tamejiro
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p. 1607 - 1610
(2007/10/02)
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- Total Syntheses of Fungal Metabolites and Functionalized Furanones
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Simple, efficient syntheses of the fungal metabolites colletochlorin D and (+/-)-ascofuranone and one of its stereoisomers are described.Our investigations of functionalized furanones also enabled us to develop a nine-step (22percent overall yield) synthe
- Chen, Kau-Ming,Semple, J. Edward,Joullie, Madeleine M.
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p. 3997 - 4005
(2007/10/02)
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- SYNTHESIS OF (+/-)-ASCOCHLORIN, (+/-)-ASCOFURANONE AND LL-Z1272α
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Three antibiotics with a common structural feature as prenylated phenols were synthesized: (+/-)-ascochlorin (5-chloro-2,4-dihydroxy-6-methyl-3-benzaldehyde), (+/-)-ascofurano
- Mori, Kenji,Fujioka, Takafumi
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p. 2711 - 2720
(2007/10/02)
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- A SIMPLE TOTAL SYNTHESIS OF (+/-)-ASCOFURANONE
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A simple, efficient total synthesis of (+/-)-ascofuranone is described.
- Chen, Kau-Ming,Joullie, Madeleine M.
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p. 3795 - 3796
(2007/10/02)
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- Synthesis of (±)-ascofuranone, an antibiotic with hypolipidemic and antitumor protective properties
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(±)-Ascofuranone, 5-chloro-2,4-dihydroxy-6-methyl-[(2E,6E)-7-(3,3-dimethyl-4-oxo-2-oxacyc lopentyl)3,7-dimethyl-2,6-heptadienyl]benzaldehyde, was synthesized.
- Mori,Fujioka
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p. 1547 - 1548
(2007/10/02)
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