- Antimycobacterial activities of 5-alkyl (or halo)-3′-substituted pyrimidine nucleoside analogs
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Several 5-alkyl (or halo)-3′-azido (amino or halo) analogs of pyrimidine nucleosides have been synthesized and evaluated against Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium. Among these compounds, 3′-azido-5-ethyl-2′,3′-dideoxyuridine (3) was found to have significant antimycobacterial activities against M. bovis (MIC 50 = 1 μg/mL), M. tuberculosis (MIC50 = 10 μg/mL) and M. avium (MIC50 = 10 μg/mL).
- Srivastav, Naveen C.,Shakya, Neeraj,Bhavanam, Sudha,Agrawal, Amogh,Tse, Chris,Desroches, Nancy,Kunimoto, Dennis Y.,Kumar, Rakesh
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p. 1091 - 1094
(2012/03/26)
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- Structure-Activity Relationships of Pyrimidine Nucleosides as Antiviral Agents for Human Immunodeficiency Virus Type 1 in Peripheral Blood Mononuclear Cells
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The structure-activity relationships of several pyrimidine nucleosides related to 3'-azido-3'-deoxythymidine (AZT) were determined in human immunodeficiency virus type 1 (HIV-1) infected human peripheral blood mononuclear cells.These studies indicated tha
- Chu, Chung K.,Schinazi, Raymond F.,Ahn, Moon K.,Ullas, Giliyar V.,Gu, Zi P.
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p. 612 - 617
(2007/10/02)
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- Pyrimidine derivatives
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Compounds of the formula STR1 wherein R1 is halogen, C1-4 -alkyl, halo-(C1-4 -alkyl) or C2-4 -alkanoyl, R2 is hydrogen, hydroxy, C1-4 alkoxy, C1-4 -alkylthio or phenyl-(C1-4 -alkoxy) or , when X is O, also acyloxy, R3 is hydrogen or C1-4 -alkyl, R4 is a carbocyclic group or a heterocyclic group, R5 is hydrogen or fluorine, m stands for zero, 1 or 2, X is O or NH and Y is a direct bond, --CH=CH--, --C C-- or a group of the formula of in which A is a C1-8 alkylene group which is optionally substituted by one or two phenyl groups, Z is O, S, SO or SO2 and n stands for zero or 1, with the proviso that R1 is different from iodine, when R2 is hydroxy or benzoyloxy, R3 is hydrogen, R4 is unsubstituted phenyl, R5 is hydrogen, m stands for zero, X is O, and Y is a direct bond, and tautomers thereof, which possess antiviral activity and can therefore be used in the form of medicaments for the control and prevention of viral infections are described. The compounds of formula I can be prepared according to known methods.
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- 2',3'-dideoxy-5-substituted uridines and related compounds as antiviral agents
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A compound which exhibits antiviral activity towards HTLV-III/LAV, having the formula: STR1 wherein R4 is O or NH; R5 is a C2-4 alkyl group or a C3-4 cycloalkyl group, wherein said alkyl group or cycloalkyl grou
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