- 6-deoxycarbovir: A xanthine oxidase activated prodrug of carbovir
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(-)-(cis)-4-(2-Amino-9H-purin-9-yl)-2-cyclopentenyl carbinol (6-deoxycarbovir) was prepared in order to evaluate prodrug approaches to increased bioavailability of the anti-HIV agent, (-)-carbovir. Incubation experiments demonstrated that 6-deoxycarbovir was rapidly converted to (-)-carbovir by the enzyme, xanthine oxidase. Since xanthine oxidase activity is present in both the intestine and liver, a high first pass conversion to carbovir would be expected in vivo.
- Vince,Brownell,Beers
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- Synthesis of 2-modified aristeromycins and their analogs as potent inhibitors against Plasmodium falciparum S-adenosyl-l-homocysteine hydrolase
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2-Modified aristeromycin derivatives and their related analogs were synthesized to investigate their inhibitory activity against human and Plasmodium falciparum S-adenosyl-l-homocysteine hydrolase (PfSAHH). 2-Fluoroaristeromycin showed a strong inhibitory activity against PfSAHH selectively and complete resistance to adenosine deaminase.
- Ando, Takayuki,Iwata, Masafumi,Zulfiqar, Fazila,Miyamoto, Tatsuya,Nakanishi, Masayuki,Kitade, Yukio
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- CYCLOPENTENYL PURINE DERIVATIVE OR SALT THEREOF
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An object of the present invention is to provide a compound exhibiting an excellent drug efficacy as an anti-adenoviral agent, and an anti-adenoviral agent. The present invention provides an anti-adenoviral agent including a compound represented by General Formula [1] (in the formula, R1 represents a hydrogen atom, a halogen atom, an amino group which may be substituted, a monocyclic nitrogen-containing heterocyclic ring group which may be substituted (provided that a nitrogen atom forming the ring is bonded to a carbon atom to which R1 is bonded), a monocyclic nitrogen- and oxygen-containing heterocyclic ring group which may be substituted (provided that a nitrogen atom forming the ring is bonded to a carbon atom to which R1 is bonded), a C1-6 alkoxy group which may be substituted, a hydroxyl group which may be protected, or the like; R2 represents a hydrogen atom or an amino protecting group; R3 represents a C1-20 alkoxy group which may be substituted, an aryloxy group which may be substituted, an amino group which may be substituted, or the like; R4 represents a C1-20 alkoxy group which may be substituted, an aryloxy group which may be substituted, an amino group which may be substituted, or the like; and X represents an oxygen atom or a sulfur atom) or a salt thereof.
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Paragraph 0296-0299
(2021/05/28)
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- PREPARATION OF SYNTHETIC NUCLEOSIDES VIA π-ALLYL TRANSITION METAL COMPLEX FORMATION
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This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof.
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Page/Page column 44; 47
(2009/04/25)
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- Analogs of (1s,cis)-4-(2-amino-9h-purin -9-yl) -2-Cyclopentene-1-methanol as antiviral
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The present invention relates to analogs of (1S, cis)-4-(2-amino-9H-purin-9-yl)-2-cyclopentene-1-methanol for use in treating viral infections.
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- Antiviral combination comprising nucleoside analogs
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Antiviral and antitumor compositions are disclosed comprising a mixture of AZT, ribavirin, d4T or CS-87 with a compound of general formula: STR1 wherein Z is H, OH or NH2, Y is CH, and X is selected from the group consisting of H, N(R)2, SR, OR or halogen, wherein R is H, lower(C1 -C4)alkyl, aryl or mixtures thereof, and the pharmaceutically-acceptable derivatives thereof.
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- Guanine derivatives having antiviral activity and their pharmaceutically acceptable salts
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Amino acid esters of carbovir have been found to have improved bioavailability after oral administration compared with carbovir. The esters are particularly useful for the treatment of hepatitis B virus and retrovirus (e.g. human immunodeficiency virus) infections. A preferred amino acid ester is the valine ester.
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- Dideoxycarbocyclic nucleosides
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Antiviral and antitumor compounds are disclosed of general formula: STR1 wherein Z is H, OH or NH2, Y is CH or N, the bond indicated by C1 '--C2 ' is absent or, in combination with the C1 '--C2 ' bond is the unit CH=CH, and X is selected from the group consisting of H, N(R2), SR, OR or halogen, wherein R is H, lower (C1 -C4)alkyl, aryl or mixtures thereof, and the pharmaceutically acceptable salts thereof.
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- Optically-active isomers of dideoxycarbocyclic nucleosides
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Antiviral and antitumor compounds are disclosed of general formula: STR1 wherein Z is H, OR' or NH2, wherein R' is H, (C1 -C4)-alkyl, aryl, CHO, (C1 -C16)alkanoyl or O=P(OH)2, Y is CH or N, and X is selected from the group consisting of H, N(R2), SR, OR' or halogen, wherein R is H, lower-(C1 -C4)alkyl, aryl or mixtures thereof, and the pharmaceutically-acceptable salts thereof.
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