(−)-6-Chloro-2-[(1-furo[2,3-<i>c</i>]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a New Broad Spectrum HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor

Wishka, Donn G.; Graber, David R.; Kopta, Laurice A.; Olmsted, Robert A.; Friis, Janice M.; Hosley, John D.; Adams, Wade J.; Seest, Eric P.; Castle, Thomas; Dolak, Lester A.; Keiser, Barbara J.; Yagi, Yoshihiko; Jeganathan, Azhwarsamy; Schlachter, Stephen T.; Murphy, Michael J.; Cleek, Gary J.; Nugent, Richard A.; Poppe, Susan M.; Swaney, Steven; Han, Fusen; Watt, W.; White, Wendy L.; Poel, Toni-Jo; Thomas, Richard; Voorman, Richard; Stefanski, Kevin; Stehle, Randall G.; Tarpley, and W. Gary; Morris, Joel

doi:10.1021/jm9801049

Cited by 45 publications

(31 citation statements)

References 17 publications

(22 reference statements)

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“…PNU-142721 possess high antiviral activity against a broad spectrum of HIV-1 variants and a favourable pharmacokinetic profile, including penetration of the blood-brain barrier in the rat. The levels of PNU-142721 found in the brain in an experiment with rats was 75% of the simultaneous plasma concentrations (Wishka et al, 1998a). (Witvrouw et al, 1998).…”

Section: Pyrimidine Thioethersmentioning

confidence: 98%

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Non-Nucleoside Reverse Transcriptase Inhibitors: The NNRTI Boom

Pedersen

1999

Antivir Chem Chemother

123

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Section: Pyrimidine Thioethersmentioning

confidence: 98%

“…These are characterized by the aralkyl group and a methyl substituent at the methylene linker. This methyl substitution introduces a stereocentre at the carbon in the methylene linker (Table 17) Wishka et al (1998a). Arranz et al (1998).…”

Section: Pyrimidine Thioethersmentioning

confidence: 99%

Non-Nucleoside Reverse Transcriptase Inhibitors: The NNRTI Boom

Pedersen

1999

Antivir Chem Chemother

123

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“…1) is an important intermediate in the synthesis of a non-nucleoside HIV reverse-transcriptase inhibitor. 6) We found that Candida maris IFO10003 has a (R)-specific reducing enzyme that reduces acetylpyridine derivatives to (R)-1-(pyridyl)ethanol derivatives with more than 99% e.e. 7) Here we describe the purification and characterization of that (R)-specific enzyme.…”

mentioning

confidence: 89%

Purification and Characterization of an NADH-Dependent Alcohol Dehydrogenase fromCandida marisfor the Synthesis of Optically Active 1-(Pyridyl)ethanol Derivatives

Kawano

Yano

Hasegawa

et al. 2011

Bioscience, Biotechnology, and Biochemistry

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“…Examples of these include DPC 083 [139] and TMC 125 [140] are excellent candidates for drug development. Other potential orally bioavailable NNRTI's include PNU-142721 [141].…”

Section: Thiocarboxanilide (Uc-781)mentioning

confidence: 99%

Anti-HIV Therapy: Current and Future Directions

Agrawal

Lu²,

Qi³

et al. 2006

CPD

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Although combinations of drugs that target the HIV reverse transcriptase and protease enzymes have clearly revolutionized the treatment of HIV/AIDS, problems with these agents, such as viral escape mutants, persistence of viral reservoirs, poor patient compliance due to complicated regimens, and toxic side effects, have emphasized the need for development of new drugs with novel mechanisms of action, as well as an HIV vaccine. Recently two new classes of drugs have been identified that interfere with the membrane fusion reaction required for HIV entry of target cells. Two such agents, T-20 (enfuvirtide) and T-1249, which have been approved by the Food and Drug Administration (FDA), block the action of the fusogenic envelope glycoprotein gp41. Others target the HIV coreceptors CCR5 and CXCR4, and are now in clinical trials. Also under development are novel agents that target the HIV integrase and HIV regulatory gene products as well as immunomodulators such as IL-12 and IL-2. This article will focus on these and other novel approaches to HIV therapeutics.

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(−)-6-Chloro-2-[(1-furo[2,3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a New Broad Spectrum HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor

Cited by 45 publications

References 17 publications

Non-Nucleoside Reverse Transcriptase Inhibitors: The NNRTI Boom

Non-Nucleoside Reverse Transcriptase Inhibitors: The NNRTI Boom

Purification and Characterization of an NADH-Dependent Alcohol Dehydrogenase fromCandida marisfor the Synthesis of Optically Active 1-(Pyridyl)ethanol Derivatives

Anti-HIV Therapy: Current and Future Directions

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