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Development of modified nucleosides that have supremely high anti-HIV activity and low toxicity and prevent the emergence of resistant HIV mutants.

Ohrui H - Proc. Jpn. Acad., Ser. B, Phys. Biol. Sci. (2011)

Bottom Line: An idea to use 4'-C-substituted-2'-deoxynucleoside derivatives was proposed based on a working hypothesis to solve the problems of existing acquired immune deficiency syndrome chemotherapy (highly active antiretroviral therapy).Subsequent studies have successfully proved the validity of the idea and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine and 2'-deoxy-4'-C-ethynyl-2-chloroadenosine, nucleoside reverse transcriptase inhibitors, which have supremely high activity against all human immunodeficiency viruses including multidrug-resistant HIV and low toxicity.

View Article: PubMed Central - PubMed

Affiliation: Yokohama College of Pharmacy, Kanagawa, Japan. h.ohrui@hamayaku.ac.jp

ABSTRACT
An idea to use 4'-C-substituted-2'-deoxynucleoside derivatives was proposed based on a working hypothesis to solve the problems of existing acquired immune deficiency syndrome chemotherapy (highly active antiretroviral therapy). Subsequent studies have successfully proved the validity of the idea and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine and 2'-deoxy-4'-C-ethynyl-2-chloroadenosine, nucleoside reverse transcriptase inhibitors, which have supremely high activity against all human immunodeficiency viruses including multidrug-resistant HIV and low toxicity.

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Related in: MedlinePlus

Body weight change of mice after a single dosage of 2′-deoxy-4′-C-ethynyl-2-fluoroadenosin, administrated orally or intravenously to ICR mice.
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC3066546&req=5

fig04: Body weight change of mice after a single dosage of 2′-deoxy-4′-C-ethynyl-2-fluoroadenosin, administrated orally or intravenously to ICR mice.

Mentions: Because 4′Ed2FA is stable to adenosine deaminase, its mouse toxicity was examined.29–31,33,35) 4′Ed2FA did not show any acute toxicity to mice by either oral or intravenous administration up to 100 mg kg−1 (Fig. 4; Table 8).


Development of modified nucleosides that have supremely high anti-HIV activity and low toxicity and prevent the emergence of resistant HIV mutants.

Ohrui H - Proc. Jpn. Acad., Ser. B, Phys. Biol. Sci. (2011)

Body weight change of mice after a single dosage of 2′-deoxy-4′-C-ethynyl-2-fluoroadenosin, administrated orally or intravenously to ICR mice.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3066546&req=5

fig04: Body weight change of mice after a single dosage of 2′-deoxy-4′-C-ethynyl-2-fluoroadenosin, administrated orally or intravenously to ICR mice.
Mentions: Because 4′Ed2FA is stable to adenosine deaminase, its mouse toxicity was examined.29–31,33,35) 4′Ed2FA did not show any acute toxicity to mice by either oral or intravenous administration up to 100 mg kg−1 (Fig. 4; Table 8).

Bottom Line: An idea to use 4'-C-substituted-2'-deoxynucleoside derivatives was proposed based on a working hypothesis to solve the problems of existing acquired immune deficiency syndrome chemotherapy (highly active antiretroviral therapy).Subsequent studies have successfully proved the validity of the idea and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine and 2'-deoxy-4'-C-ethynyl-2-chloroadenosine, nucleoside reverse transcriptase inhibitors, which have supremely high activity against all human immunodeficiency viruses including multidrug-resistant HIV and low toxicity.

View Article: PubMed Central - PubMed

Affiliation: Yokohama College of Pharmacy, Kanagawa, Japan. h.ohrui@hamayaku.ac.jp

ABSTRACT
An idea to use 4'-C-substituted-2'-deoxynucleoside derivatives was proposed based on a working hypothesis to solve the problems of existing acquired immune deficiency syndrome chemotherapy (highly active antiretroviral therapy). Subsequent studies have successfully proved the validity of the idea and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine and 2'-deoxy-4'-C-ethynyl-2-chloroadenosine, nucleoside reverse transcriptase inhibitors, which have supremely high activity against all human immunodeficiency viruses including multidrug-resistant HIV and low toxicity.

Show MeSH
Related in: MedlinePlus