- African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase
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African trypanosomiasis is a parasitic disease affecting 5000 humans and millions of livestock animals in sub-Saharan Africa every year. Current treatments are limited, difficult to administer and often toxic causing long term injury or death in many pati
- West, Ryan A.,O'Doherty, Oran G.,Askwith, Trevor,Atack, John,Beswick, Paul,Laverick, Jamie,Paradowski, Michael,Pennicott, Lewis E.,Rao, Srinivasa P.S.,Williams, Gareth,Ward, Simon E.
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p. 676 - 689
(2017/11/01)
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- 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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- COMPOUNDS FOR USE AS INHIBITORS OF ALTERNATIVE OXIDASE OR CYTOCHROME BC1 COMPLEX
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The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infe
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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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Paragraph 0120; 0121
(2013/09/26)
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- A general approach for the synthesis of phenolic natural products. Facile syntheses of grifolin and colletochlorins B and D
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A general approach is established for the synthesis of phenolic compounds having terpenoid side chains: (1) protection of the phenolic hydroxyls in the aromatic precursor by ether formation, (2) coupling the aromatic part with a terpenoid bromide, and (3) deprotection to regenerate the hydroxyl groups. This strategy was successfully applied to the synthesis of colletochlorins B and D and grifolin. Some of the colletochlorin derivatives were found to inhibit the cell growth of P388.
- Saimoto,Ueda,Sashiwa,Shigemasa,Hiyama
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p. 1178 - 1185
(2007/10/02)
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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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- A GENERAL HIGHLY EFFICIENT ACCESS TO PRENYLATED PHENOLIC NATURAL PRODUCTS. SYNTHESIS OF COLLETOCHLORINS B AND D
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A general approach is reported for the synthesis of phenolic natural products having terpenoid side chains: (1) construction of the requisite bromophenol ethers, (2) coupling the aromatic ring with a terpenoid chain through copper(I) ate complex, and (3)
- Saimoto, Hiroyuki,Hiyama, Tamejiro
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p. 597 - 600
(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 GENERAL SYNTHETIC METHOD FOR PRENYLATED PHENOLS OF MICROBIAL ORIGIN
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Prenylated phenols with a fully substituted benzene ring, such as colletochlorins A and B, were synthesized by first prenylating 1,5-dimethoxy-3-methyl-1,4-cyclohexadiene and then effecting the aromatization of the prenylated product.
- Mori, Kenji,Sato, Kazuo
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p. 1221 - 1225
(2007/10/02)
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