Search Results - "Weatherhead, Jason"

Carbamoyl Pyridone HIV‑1 Integrase Inhibitors 3. A Diastereomeric Approach to Chiral Nonracemic Tricyclic Ring Systems and the Discovery of Dolutegravir (S/GSK1349572) and (S/GSK1265744) by Johns, Brian A, Kawasuji, Takashi, Weatherhead, Jason G, Taishi, Teruhiko, Temelkoff, David P, Yoshida, Hiroshi, Akiyama, Toshiyuki, Taoda, Yoshiyuki, Murai, Hitoshi, Kiyama, Ryuichi, Fuji, Masahiro, Tanimoto, Norihiko, Jeffrey, Jerry, Foster, Scott A, Yoshinaga, Tomokazu, Seki, Takahiro, Kobayashi, Masanori, Sato, Akihiko, Johnson, Matthew N, Garvey, Edward P, Fujiwara, Tamio

“…We report herein the discovery of the human immunodeficiency virus type-1 (HIV-1) integrase inhibitors dolutegravir (S/GSK1349572) (3) and S/GSK1265744 (4)…”
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Carbamoyl Pyridone HIV‑1 Integrase Inhibitors. 2. Bi- and Tricyclic Derivatives Result in Superior Antiviral and Pharmacokinetic Profiles by Kawasuji, Takashi, Johns, Brian A, Yoshida, Hiroshi, Weatherhead, Jason G, Akiyama, Toshiyuki, Taishi, Teruhiko, Taoda, Yoshiyuki, Mikamiyama-Iwata, Minako, Murai, Hitoshi, Kiyama, Ryuichi, Fuji, Masahiro, Tanimoto, Norihiko, Yoshinaga, Tomokazu, Seki, Takahiro, Kobayashi, Masanori, Sato, Akihiko, Garvey, Edward P, Fujiwara, Tamio

“…This work is a continuation of our initial discovery of a potent monocyclic carbamoyl pyridone human immunodeficiency virus type-1 (HIV-1) integrase inhibitor…”
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The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore by Johns, Brian A., Weatherhead, Jason G., Allen, Scott H., Thompson, James B., Garvey, Edward P., Foster, Scott A., Jeffrey, Jerry L., Miller, Wayne H.

“…A series of HIV-1 integrase inhibitors containing a novel metal binding motif consisting of the 8-hydroxy-1,6-naphthyridine core and either an oxadiazole or…”
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1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position by Johns, Brian A., Weatherhead, Jason G., Allen, Scott H., Thompson, James B., Garvey, Edward P., Foster, Scott A., Jeffrey, Jerry L., Miller, Wayne H.

“…The use of a 1,3,4-oxadiazole in combination with an 8-hydroxy-1,6-naphthyridine ring system has been shown to deliver potent enzyme and antiviral activity…”
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Synthesis and pharmacokinetic profile of highly deuterated brecanavir analogs by Velthuisen, Emile J., Baughman, Todd M., Johns, Brian A., Temelkoff, David P., Weatherhead, Jason G.

“…Several highly deuterated analogs of the HIV-1 protease inhibitor brecanavir have been prepared to study the effect of deuterium upon metabolic stability. The…”
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The Naphthyridinone GSK364735 Is a Novel, Potent Human Immunodeficiency Virus Type 1 Integrase Inhibitor and Antiretroviral by GARVEY, Edward P, JOHNS, Brian A, WEATHERHEAD, Jason G, KOBLE, Cecilia S, ALIEN, Scott H, SCHALLER, Lee T, SHERRILL, Ronald G, YOSHINAGA, Tomokazu, KOBAYASHI, Masanori, WAKASA-MORIMOTO, Chiaki, MIKI, Shigeru, NAKAHARA, Koichiro, GARTLAND, Margaret J, NOSHI, Takeshi, SATO, Akihiko, FUJIWARA, Tamio, FOSTER, Scott A, MILLER, Wayne H, FERRIS, Robert G, HAZEN, Richard J, UNDERWOOD, Mark R, BOROS, Eric E, THOMPSON, James B

“…ERRATUM ( vol. 52 , p. 1899 ) Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg…”
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Naphthyridinone (NTD) integrase inhibitors: N1 Protio and methyl combination substituent effects with C3 amide groups by Johns, Brian A., Kawasuji, Takashi, Weatherhead, Jason G., Boros, Eric E., Thompson, James B., Koble, Cecilia S., Garvey, Edward P., Foster, Scott A., Jeffrey, Jerry L., Fujiwara, Tamio

“…Substituent effects of a series of N1 protio and methyl naphthyridinone HIV-1 integrase strand-transfer inhibitors has been explored. The effects of…”
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Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups by Johns, Brian A., Kawasuji, Takashi, Weatherhead, Jason G., Boros, Eric E., Thompson, James B., Koble, Cecilia S., Garvey, Edward P., Foster, Scott A., Jeffrey, Jerry L., Fujiwara, Tamio

“…A series of N1 acetamide substituted naphthyridinone HIV-1 integrase inhibitors have been explored to understand structure–activity relationships (SAR) with…”
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Pharmacovirological Impact of an Integrase Inhibitor on Human Immunodeficiency Virus Type 1 cDNA Species In Vivo by GOFFINET, Christine, ALLESPACH, Ina, KEPPLER, Oliver T, OBERBREMER, Lena, GOLDEN, Pamela L, FOSTER, Scott A, JOHNS, Brian A, WEATHERHEAD, Jason G, NOVICK, Steven J, CHISWELL, Karen E, GARVEY, Edward P

“…Article Usage Stats Services JVI Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Combining symmetry elements results in potent naphthyridinone (NTD) HIV-1 integrase inhibitors by Johns, Brian A., Kawasuji, Takashi, Weatherhead, Jason G., Boros, Eric E., Thompson, James B., Garvey, Edward P., Foster, Scott A., Jeffrey, Jerry L., Miller, Wayne H., Kurose, Noriyuki, Matsumura, Kenichi, Fujiwara, Tamio

“…A series of naphthyridinone HIV-1 integrase strand-transfer inhibitors have been designed based on a psdeudo-C2 symmetry element present in the two-metal…”
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The Naphthyridinone GSK364735 Is a Novel, Potent Human Immunodeficiency Virus Type 1 Integrase Inhibitor and Antiretroviral by Garvey, Edward P, Johns, Brian A, Gartland, Margaret J, Foster, Scott A, Miller, Wayne H, Ferris, Robert G, Hazen, Richard J, Underwood, Mark R, Boros, Eric E, Thompson, James B, Weatherhead, Jason G, Koble, Cecilia S, Allen, Scott H, Schaller, Lee T, Sherrill, Ronald G, Yoshinaga, Tomokazu, Kobayashi, Masanori, Wakasa-Morimoto, Chiaki, Miki, Shigeru, Nakahara, Koichiro, Noshi, Takeshi, Sato, Akihiko, Fujiwara, Tamio

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Pyrazolopyrimidines and pyrazolotriazines with potent activity against herpesviruses by Gudmundsson, Kristjan S., Johns, Brian A., Weatherhead, Jason

“…Synthesis of several pyrazolo[1,5- c]pyrimidines, pyrazolo[1,5- a]pyrimidines and pyrazolo[1,5- a][1,3,5]triazines with potent activity against herpes simplex…”
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Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase by Maynard, Andrew, Crosby, Renae M., Ellis, Byron, Hamatake, Robert, Hong, Zhi, Johns, Brian A., Kahler, Kirsten M., Koble, Cecilia, Leivers, Anna, Leivers, Martin R., Mathis, Amanda, Peat, Andrew J., Pouliot, Jeffrey J., Roberts, Christopher D., Samano, Vicente, Schmidt, Rachel M., Smith, Gary K., Spaltenstein, Andrew, Stewart, Eugene L., Thommes, Pia, Turner, Elizabeth M., Voitenleitner, Christian, Walker, Jill T., Waitt, Greg, Weatherhead, Jason, Weaver, Kurt, Williams, Shawn, Wright, Lois, Xiong, Zhiping Z., Haigh, David, Shotwell, J. Brad

“…A boronic acid moiety was found to be a critical pharmacophore for enhanced in vitro potency against wild-type hepatitis C replicons and known clinical…”
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